Drug development for Malaria: novel approaches for prevention and treatment
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| Weitere Verfasser: | |
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| Format: | Buch |
| Sprache: | English |
| Veröffentlicht: |
Weinheim
Wiley-VCH
[2023]
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| Schlagworte: | |
| Online-Zugang: | Inhaltsverzeichnis |
| Beschreibung: | xiv, 378 Seiten Illustrationen, Diagramme |
| ISBN: | 9783527348602 |
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MARC
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| 001 | BV047958174 | ||
| 003 | DE-604 | ||
| 005 | 20221212 | ||
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| 008 | 220427s2023 gw a||| |||| 00||| eng d | ||
| 016 | 7 | |a 1241347468 |2 DE-101 | |
| 020 | |a 9783527348602 |9 978-3-527-34860-2 | ||
| 035 | |a (OCoLC)1355305612 | ||
| 035 | |a (DE-599)DNB1241347468 | ||
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| 084 | |8 1\p |a 540 |2 23sdnb | ||
| 245 | 1 | 0 | |a Drug development for Malaria |b novel approaches for prevention and treatment |c edites by Pravin Kendrekar |
| 264 | 1 | |a Weinheim |b Wiley-VCH |c [2023] | |
| 300 | |a xiv, 378 Seiten |b Illustrationen, Diagramme | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
| 338 | |b nc |2 rdacarrier | ||
| 650 | 0 | 7 | |a Arzneimittelentwicklung |0 (DE-588)4143176-5 |2 gnd |9 rswk-swf |
| 650 | 0 | 7 | |a Antimalariamittel |0 (DE-588)4142684-8 |2 gnd |9 rswk-swf |
| 653 | |a Biowissenschaften | ||
| 653 | |a Chemie | ||
| 653 | |a Chemistry | ||
| 653 | |a Drug Discovery & Development | ||
| 653 | |a Infectious Disease | ||
| 653 | |a Infektionskrankheiten | ||
| 653 | |a Life Sciences | ||
| 653 | |a Medical Science | ||
| 653 | |a Medizin | ||
| 653 | |a Parasitologie | ||
| 653 | |a Parasitology | ||
| 653 | |a Wirkstoffforschung u. -entwicklung | ||
| 653 | |a CH61: Wirkstoffforschung u. -entwicklung | ||
| 653 | |a LSE0: Parasitologie | ||
| 653 | |a MDD2: Infektionskrankheiten | ||
| 655 | 7 | |0 (DE-588)4143413-4 |a Aufsatzsammlung |2 gnd-content | |
| 689 | 0 | 0 | |a Antimalariamittel |0 (DE-588)4142684-8 |D s |
| 689 | 0 | 1 | |a Arzneimittelentwicklung |0 (DE-588)4143176-5 |D s |
| 689 | 0 | |5 DE-604 | |
| 700 | 1 | |a Kendrekar, Pravin |0 (DE-588)1271144336 |4 edt | |
| 776 | 0 | 8 | |i Erscheint auch als |n Online-Ausgabe, PDF |z 978-3-527-83060-2 |
| 776 | 0 | 8 | |i Erscheint auch als |n Online-Ausgabe, EPUB |z 978-3-527-83059-6 |
| 776 | 0 | 8 | |i Erscheint auch als |n Online-Ausgabe, oBook |z 978-3-527-83058-9 |
| 856 | 4 | 2 | |m DNB Datenaustausch |q application/pdf |u http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=033339420&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |3 Inhaltsverzeichnis |
| 999 | |a oai:aleph.bib-bvb.de:BVB01-033339420 | ||
| 883 | 1 | |8 1\p |a vlb |d 20210917 |q DE-101 |u https://d-nb.info/provenance/plan#vlb | |
Datensatz im Suchindex
| _version_ | 1804183645702848512 |
|---|---|
| adam_text | CONTENTS
PART
1
INTRODUCTION
1
1
CHRONOLOGY
OF
DRUG
DEVELOPMENT
FOR
MALARIA
3
NALINI
KURUP
AND
NIKHIL
RAJNANI
1.1
1.1.1
1.2
1.2.1
1.3
1.3.1
1.4
1.4.1
1.5
1.6
1.6.1
1.7
1.7.1
INTRODUCTION
3
LIFE
CYCLE
OF
MALARIA
(ADAPTED
FROM
CDC)
4
MALARIA
-
ERSTWHILE
MEMORIES
5
PROGRESS
FIGHTING
MALARIA
5
CURRENT
CHEMOTHERAPY
USED
TO
TREAT
MALARIA
7
CURRENT
COMBINATION
THERAPY
13
DRUG
RESISTANCE
OF
ANTIMALARIAL
DRUGS
14
DETECTION
OF
DRUG
RESISTANCE
16
NEWER
DRUGS
APPROVED
FOR
MALARIA
TREATMENT
17
CURRENT
APPROACHES
TO
DEVELOPING
A
MALARIA
VACCINE
18
HOPE
FOR
VACCINE
LIES
IN
THE
PARASITE
ITSELF
18
CONCLUSION:
THE
PATH
FORWARD
20
RTS,
-S
VACCINE:
A
NEW
TOOL
WITH
POTENTIAL
FOR
AFRICA
20
REFERENCES
21
PART
II
CHALLENGES
AND
OPPORTUNITIES
IN
MALARIA
THERAPY
25
2
SCIENTIFIC
CHALLENGES
AND
TREATMENT
OPPORTUNITIES
IN
THE
FACE
OF
SHIFTING
MALARIA
EPIDEMIOLOGY
27
KETAKI
RAMANI
2.1
2.2
2.3
2.3.1
2.3.2
2.3.2.1
2.3.2.2
INTRODUCTION
27
THE
SCIENTIFIC
CHALLENGES
AGAINST
MALARIAL
DRUG
28
ADVANCES
IN
UNDERSTANDING
AND
MANAGING
DRUG
RESISTANCE
29
VECTOR
AND
ITS
CONTROL
29
PARASITE
AND
ITS
CONTROL
30
MALARIA
VACCINE
31
ANTIMALARIAL
DRUGS
31
VI
CONTENTS
2.4
2.4.1
2.4.2
2.5
2.6
METHODS
TO
ASSESS
THE
PRESENCE
AND
LEVEL
OF
DRUG
RESISTANCE
32
THERAPEUTIC
EFFICACY
OF
ANTIMALARIAL
DRUGS
32
MOLECULAR
MARKERS
ASSOCIATED
WITH
P.
FALCIPARUM
33
ANTIMALARIAL
DRUGS
CURRENTLY
IN
USE
AND
IN
THE
PIPELINE
33
FUTURE
38
REFERENCES
40
3
EMERGING
FORMULATION
TECHNOLOGIES
AGAINST
MALARIA
RESURGENCE
45
KINJAL
PARIKH,
RAKHEE
KAPADIA,
ROHAN
PAI,
MAHENDRA
PRAJAPATI,
AND
GANESH
SHEVALKAR
LIST
OF
ABBREVIATIONS
45
3.1
3.1.1
3.1.2
3.2
3.2.1
3.2.2
3.2.3
3.2.4
3.3
INTRODUCTION
46
MAJOR
PATHOLOGICAL
HALLMARKS
OF
MALARIA
46
CURRENT
TREATMENT
STRATEGIES
47
PITFALLS
OF
THE
CURRENT
TREATMENT
REGIMEN
47
DRUG
RESISTANCE
47
HIGH
DRUG
DOSE
48
LONG-TERM
TREATMENT
48
RECURRENCE
AND
REVERSION
OF
DISEASES
48
NANOTECHNOLOGY-BASED
STRATEGIES
FOR
TARGETING
IN
ANTIMALARIAL
THERAPY
49
3.3.1
3.3.2
3.3.2.1
3.3.2.2
3.3.2.3
3.3.3
3.4
3.4.1
3.4.1.1
3.4.1.2
3.4.1.3
PASSIVE
TARGETING
49
ACTIVE
TARGETING
49
HEPATOCYTE
TARGETING
50
ERYTHROCYTE
TARGETING
50
BRAIN
TARGETING
50
RAPID
DIAGNOSIS
AND
VECTOR
CONTROL
51
NANO
FORMULATIONS
FOR
MALARIAL
TREATMENT
51
LIPID-BASED
NANOPLATFORMS
52
NANOEMULSION
52
SELF-EMULSIFYING
DRUG
DELIVERY
SYSTEM
(SEDDS)
53
SOLID
LIPID
NANOPARTICLES
(SLNS)
AND
NANOSTRUCTURED
LIPID
CARRIERS
(NLCS)
54
3.4.1.4
3.4.2
3.4.2.1
3.4.2.2
3.4.2.3
3.4.2.4
3.4.2.5
3.4.2.6
3.4.3
3.4.4
3.4.4.1
LIPOSOME
54
POLYMER-BASED
NANOPLATFORMS
FOR
MALARIA
55
NANOPARTICLES
55
NANOCAPSULES
58
DENDRIMERS
58
MICELLES
59
POLYMERIC
HYDROGEL
NANOPARTICLES
59
NANOSUSPENSION
59
ORGANIZED
LAYER-BY-LAYER
ASSEMBLY
59
INORGANIC
NANO-ARCHITECTONICS
59
METALLIC
PLATFORMS
60
CONTENTS
VII
3.4.4.2
3.4.4.3
3.4.4.4
3.4.5
3.4.5.1
3.4.5.2
3.4.6
3.4.7
3.4.7.1
3.4.7.2
3.4.7.3
3.4.7.4
3.5
3.5.1
QUANTUM
DOTS
61
CARBON
NANOSTRUCTURES
62
BIO-CERAMICS
62
BIO-INSPIRED
NANOCARRIERS
63
VACCINES
BASED
ON
BIO-INSPIRED
NANOCARRIERS
63
BIO-ENGINEERED
STRATEGY
BASED
ON
ERYTHROCYTES
64
PROTEIN-PEPTIDE-BASED
DRUG
DELIVERY
SYSTEM
64
STIMULI-RESPONSIVE
PLATFORMS
FOR
MALARIA
64
PH-RESPONSIVE
FORMULATIONS
65
THERMO-RESPONSIVE
FORMULATIONS
65
REDOX
STATE
RESPONSIVE
SUBSTANCES
65
STIMULI-RESPONSIVE
LIQUID
CRYSTALLINE
MATERIALS
65
DIAGNOSTICS
66
STIMULI-RESPONSIVE
IRON
OXIDE
AND
GOLD
NANOPARTICLE
REAGENT
SYSTEM
66
3.5.2
3.5.3
3.6
3.6.1
3.6.2
3.6.3
3.6.4
IMMUNOLOGICAL
ADJUVANTS
66
NANOFIBERS
66
CHALLENGES
IN
CLINICAL
TRANSLATION
OF
NANOMEDICINE
67
BIOLOGICAL
CHALLENGES
67
BIOCOMPATIBILITY
AND
SAFETY
67
CHALLENGES
IN
MANUFACTURING
SCALE-UP
AND
REPRODUCIBILITY
67
ANALYTICAL
CHARACTERIZATION
AND
QUALITY
CONTROL
CHALLENGES
OF
NANO-FORMULATIONS
68
3.6.5
3.6.6
3.7
3.8
REGULATORY
CHALLENGES
68
OTHER
CHALLENGES
69
SUMMARY
AND
FUTURE
PERSPECTIVE
69
CONCLUSION
69
ACKNOWLEDGMENTS
70
REFERENCES
70
4
TARGETED
DRUG
DELIVERY
FOR
ANTIMALARIAL
THERAPY
83
SUHA
ZWAYEN,
TAMARA
ZWAIN,
AND
KAMALINDER
K.
SINGH
4.1
4.2
4.2.1
4.2.2
4.2.3
4.3
4.4
4.4.1
4.4.2
4.4.3
4.4.4
4.4.5
4.5
INTRODUCTION
83
REMODELLING
OF
PARASITE-INFECTED
RED
BLOOD
CELL
(PRBC)
84
THE
RED
BLOOD
CELL
MEMBRANE
(RBCM)
85
THE
PARASITOPHOROUS
VACUOLE
MEMBRANE
(PVM)
85
THE
PARASITE
PLASMA
MEMBRANE
(PPM)
86
THE
EMERGENCE
OF
RESISTANCE
AND
ANTIMALARIAL
THERAPY
APPROACH
86
NANOCARRIERS
FOR
ANTIMALARIAL
DRUG
DELIVERY
89
LIPOSOMES
89
SOLID
LIPID
NANOPARTICLES
(SLNS)
91
NANOSTRUCTURED
LIPID
CARRIERS
(NLCS)
91
NANO-EMULSIONS
(NES)
91
POLYMERIC
NANOPARTICLES
92
TARGETED
ANTIMALARIAL
DRUG
DELIVERY
SYSTEMS
92
VIII
CONTENTS
4.5.1
4.5.2
4.6
PASSIVE
DRUG
TARGETING
WITH
CONVENTIONAL
NANOCARRIERS
92
ACTIVE
DRUG
TARGETING
WITH
SURFACE-MODIFIED
NANOCARRIER
93
CONCLUSION:
MOVING
TOWARDS
THE
FUTURE
97
ACKNOWLEDGEMENTS
97
REFERENCES
97
5
THE
IMMINENT
THREAT
OF
ANTIMALARIAL
DRUG
RESISTANCE
105
BHARTI
SINGAL
AND
JYOTI
CHHIBBER-GOEL
5.1
5.2
5.3
5.3.1
5.3.2
5.3.3
5.3.4
5.4
5.4.1
5.4.2
5.4.3
5.4.3.1
5.4.3.2
5.4.4
5.4.4.1
5.4.4.2
5.5
5.5.1
5.5.2
5.5.3
5.6
INTRODUCTION
105
ANTIMALARIAL
DRUGS:
AN
OVERVIEW
107
THE
EVOLUTION
OF
CQ
RESISTANCE
109
MECHANISM
OF
ACTION
OF
CQ
109
BASIS
OF
CQ
RESISTANCE
110
PREVALENCE
OF
CQ
RESISTANCE
112
WHO
GUIDELINES
TO
USE
CQ
113
IMPACT
OF
SULFADOXINE-PYRIMETHAMINE
RESISTANCE
113
MECHANISM
OF
ACTION
OF
SP
114
SP
RESISTANCE
116
DISTRIBUTION
OF
DHPS
AND
DHFR
MUTATION
ACROSS
GLOBE
117
DHFR
117
DHPS
117
WHO
GUIDELINES
TO
USE
SP
118
IPTP
GUIDELINES
118
IPTI
GUIDELINES
118
ACT
RESISTANCE
118
MECHANISM
OF
ACTION
OF
ART
121
ART
RESISTANCE
AND
ACT
FAILURE
122
WHO
GUIDELINES
123
CONCLUSION:
THE
ROAD
AHEAD
124
REFERENCES
124
6
CURRENT
THERAPIES
AND
NEW
DRUG
TARGETS
FOR
THE
FUTURE
DRUG
DEVELOPMENT
OF
DRUG
RESISTANT
MALARIA
133
POOJA
MITTAL
AND
RUPESH
K.
GAUTAM
6.1
6.2
6.3
6.4
6.4.1
6.4.1.1
6.4.1.2
6.4.1.3
6.4.1.4
6.4.2
INTRODUCTION
133
LIFE
CYCLE
OF
PLASMODIUM
FALCIPARUM
134
CURRENT
ANTIMALARIAL
THERAPY
AND
THEIR
SHORTCOMINGS
134
DRUG
TARGETS
FOR
CURRENT
ANTIMALARIAL
THERAPY
136
DRUG-RESISTANT
MALARIA
AND
IDENTIFICATION
OF
NEW
TARGETS
137
FOOD
VACUOLE
AS
DRUG
TARGETS
137
SHIKIMIC
ACID
PATHWAY
TARGETING
142
TARGETING
FOLATE
PATHWAY
AND
METHIONINE
SYNTHESIS
PATHWAY
142
GLYCOLYTIC
PATHWAY
INHIBITION
144
MITOCHONDRIA
AS
DRUG
TARGETS
144
CONTENTS
IX
6.4.2.1
6.4.2.2
6.5
6.5.1
6.5.2
6.5.3
6.5.4
6.5.5
6.6
TARGETING
ELECTRON
TRANSPORT
CHAIN
144
INHIBITION
OF
DIHYDROORATE
DEHYDROGENASE
144
FUTURE
DRUG
DEVELOPMENT
FOR
THE
TREATMENT
OF
MALARIA
146
BENEFITS
OF
NANOCARRIERS
146
LIPID-BASED
DRUG
DELIVERY
146
LIPOSOMES (AS
NANOCARRIERS)
146
NANOSTRUCTURED
LIPID
CARRIERS
146
SOLID
LIPID
NANOCARRIERS
147
CONCLUSION
147
REFERENCES
147
PART
III
DRUG
DEVELOPMENT
151
7
ASSAYS
FOR
ANTIMALARIAL
DRUG
DISCOVERY
153
VARUN
GORKI,
NEHA
S.
WALTER,
AND
SUKHBIR
KAUR
7.1
7.2
7.2.1
7.2.2
7.2.3
7.2.4
INTRODUCTION
153
IN
VITRO
ASSAYS
FOR
ANTIMALARIAL
DRUG
DISCOVERY
155
SCHIZONT
MATURATION
INHIBITION
ASSAY
(MICROSCOPIC
TEST)
156
IN
VITRO
MICRO
TEST
TECHNIQUE
156
RADIOISOTOPE
ASSAY
156
COLORIMETRIC
ASSAY
(PLASMODIUM
LACTATE
DEHYDROGENASE
ASSAY
[PLDH])
157
7.2.5
7.2.5.1
7.2.5.2
7.2.6
7.2.7
7.2.8
7.2.9
7.2.10
7.2.11
ELISA-BASED
METHODS
157
DELI
ASSAY
157
ASSAY
BASED
ON
HISTIDINE-RICH
PROTEIN
II
(HRPII)
OF
P.
FALCIPARUM
158
FLOW
CYTOMETRY
158
FLUOROMETRIC
ASSAY
158
0-HEMATIN
FORMATION
(HAEMOZOIN
TEST)
159
DRUG
INTERACTION
ASSAY
AND
ISOBOLOGRAM
ANALYSIS
159
PCR-BASED
METHODS
160
IN
VITRO
ASSAYS
TARGETING EXO-ERYTHROCYTIC
AND
SEXUAL
STAGES
OF
THE
PARASITE
160
7.2.11.1
7.2.11.2
7.3
7.3.1
7.3.2
7.3.3
7.3.4
7.3.5
7.3.6
7.3.7
7.3.8
EXO-ERYTHROCYTIC
SCHIZONTOCIDAL
ASSAY
160
EX-FLAGELLATION
ASSAY
160
IN
VIVO
ASSAYS
FOR
ANTIMALARIAL
DRUG
DISCOVERY
161
PETERS
4-DAY
TEST
162
DOSE
RANGING
FULL
4-DAY
TEST
163
ONSET/RECRUDESCENCE
TEST
163
PREVENTIVE
TEST
166
CURATIVE
TEST
166
HILL
S
TEST
FOR
CAUSAL
PROPHYLAXIS
AND
RESIDUAL
ACTIVITY
166
ASSAYS
WITH
P.
BERGHEI
GREEN
FLUORESCENT
PROTEIN
(PBGFP)
167
ASSAYS
EMPLOYING
IMMUNOCOMPROMISED
MICE
167
X
CONTENTS
7.3.9
7.3.10
7.3.11
7.4
7.5
7.5.1
7.5.2
7.5.3
7.5.4
7.5.5
7.6
7.6.1
7.6.1.1
7.6.1.2
7.6.2
7.7
PRIMATE
MODELS
FOR
IN
VIVO
STUDIES
168
SPORONTOCIDAL
ASSAYS
169
ANTI-SPOROZOITE
ASSAY
169
EX
VIVO
ASSAYS
FOR
ANTIMALARIAL
DRUG
DISCOVERY
169
ASSAYS
FOR
ASSESSMENT
OF
IN
VITRO
TOXICITY
170
MTT
ASSAY
170
XTT
ASSAY
172
LDH
(LACTATE
DEHYDROGENASE)
ASSAY
172
PROTEIN
CONTENT
ASSAY
173
NEUTRAL
RED
UPTAKE
ASSAY
(NRU)
173
ASSAYS
FOR
ASSESSMENT
OF
IN
VIVO
TOXICITY
173
ACUTE
TOXICITY
174
LIMIT
TEST
OF
LORKE
175
UP
AND
DOWN
PROCEDURE
175
CHRONIC
TOXICITY
175
CONCLUSION
176
REFERENCES
177
8
AMINOACYL-TRNA
SYNTHETASES
AS
MALARIAL
DRUG
TARGETS:
A
STRUCTURAL
BIOLOGY
PERSPECTIVE
187
BHARTI
SINGAL
AND
JYOTI
CHHIBBER-GOEL
8.1
8.2
8.2.1
8.2.2
8.3
8.4
8.4.1
8.4.2
8.4.3
8.4.4
8.5
8.5.1
8.5.2
8.6
8.6.1
8.7
8.7.1
8.7.2
8.8
8.9
INTRODUCTION
187
PF/PV^BES
188
PF/PV
GENOME
188
AMINOACYL-TRNA
SYNTHETASES
(AARSS)
189
AMINOACYL-TRNA
SYNTHETASES
AS
DRUGGABLE
TARGETS
190
BIOCHEMICAL
SCREENING
OF
DRUG
LIBRARIES
192
COLORIMETRIC
ASSAYS
192
ENZYME
COUPLED
ASSAYS
193
LUCIFERASE
ASSAY
193
ASSAY
TO
TEST
SYNTHETIC
AS
WELL
AS
PROOFREADING
ACTIVITY
193
STRUCTURALLY
VALIDATED
PF/PV-AARSS
AS
DRUG
TARGETS
194
LYSYL-TRNA
SYNTHETASE
(KRS)
194
PROLYL-TRNA
SYNTHETASE
197
POTENTIAL
DRUG
TARGETS
PF/PV-AARSS
199
LEUCYL-TRNA
SYNTHETASE
(LRS)
199
ARGINYL-TRNA
SYNTHETASE
(RRS)
199
TRYPTOPHANYL-TRNA
SYNTHETASE
(WRS)
201
TYROSYL-TRNA
SYNTHETASE
202
OTHERS
203
CONCLUSION:
THE
ROAD
AHEAD
203
REFERENCES
204
CONTENTS
|
XI
9
NATURAL
PRODUCTS
AS
A
SOURCE
FOR
ANTIMALARIAL
DRUG
DEVELOPMENT
PROCESS
-
AN
OVERVIEW
213
UMA
R.
LAL
AND
SNIGDHA
LAL
9.1
INTRODUCTION
213
9.2
PHYTOCHEMICALS
AS
ANTIMALARIAL
AGENTS:
RECENT
DEVELOPMENTS
214
9.2.1
ALKALOIDS
214
9.2.2
TERPENES
219
9.2.2.1
SESQUITERPENE
LACTONES
219
9.2.2.2
DITERPENES
220
9.2.2.3
TRITERPENES
222
9.2.2.4
STEROIDS
AND
OTHERS
224
9.2.3
POLYPHENOLS
224
9.2.3.1
BIFLAVONOIDS
224
9.2.3.2
PRENYLATED
FLAVONOIDS
226
9.2.3.3
OTHER
FLAVONOIDS
226
9.3
TRADITIONAL
SYSTEM
OF
MEDICINE
AND
MALARIA
227
9.3.1
PLANTS/FORMULATIONS
USED
IN
MALARIA
TREATMENT
IN
AYURVEDIC
SYSTEM
OF
MEDICINE
227
9.4
CONCLUSIONS
228
REFERENCES
228
10
MUSHROOM-DERIVED
PRODUCTS
AS
AN
ALTERNATIVE
ANTIMALARIAL
THERAPEUTICS:
A
REVIEW
235
SENZOSENKOSI
S.
MKHIZE,
KGOTHATSO
E.
MACHABA,
MTHOKOZISI
B.
C.
SIMELANE,
AND
OFENTSE
J.
POOE
10.1
INTRODUCTION
235
10.2
BIOLOGICAL
ROLES
OF
MUSHROOMS
235
10.2.1
MALARIAL
HISTORY
AND
IMPACT
235
10.2.2
ANTIMALARIAL
ACTIVITY
OF
MUSHROOM
EXTRACTS
237
10.2.3
BIOACTIVE
MOLECULES
FOUND
WITHIN
MUSHROOMS
239
10.2.4
PHYTOCHEMICAL
PROPERTIES
OF
MUSHROOM
DERIVED
ANTIMALARIAL
PRODUCTS
241
10.2.5
IMMUNOMODULATORY
PROPERTIES
OF
MUSHROOMS
243
10.3
CONCLUSION
243
ACKNOWLEDGEMENTS
244
REFERENCES
244
11
DISCOVERY
AND
TRENDS
OF
8-AMINOQUINOLINE
AND
4-AMINOQUINOLINE
CLASSES
OF
ANTIMALARIALS
251
MEENAKSHI
JAIN,
SAMARPITA
DAS,
AND
RAHUL
JAIN
11.1
INTRODUCTION
251
11.1.1
HISTORY
251
XII
CONTENTS
11.1.2
11.1.3
11.1.3.1
11.1.3.2
11.2
MODE
OF
ACTION
253
SAR
OF
AMINOQUINOLINES
255
SAR
OF
8-AMINOQUINOLINES
255
SAR
OF
4
AMINOQUINOLINES
257
SYNTHETIC
APPROACHES
OF
8-AMINOQUINOLINES
AND
4-AMINOQUINOLINES
259
11.2.1
11.2.1.1
11.2.1.2
11.2.2
11.2.2.1
11.2.2.2
11.3
SYNTHETIC
APPROACH
OF
8-AMINOQUINOLINES
259
SYNTHETIC
APPROACH
OF
WELL-ESTABLISHED
DRUGS
259
SYNTHETIC
APPROACH
OF
RECENTLY
DEVELOPED
PQ
CONGENERS
269
SYNTHETIC
APPROACHES
OF
4-AMINOQUINOLINES
270
SYNTHETIC
APPROACHES
TO
WELL-ESTABLISHED
DRUGS
270
SYNTHETIC
APPROACH
OF
PQ-CQ
HYBRID
280
CONCLUSION
AND
FUTURE
PERSPECTIVES
280
ACKNOWLEDGMENT
281
REFERENCES
281
12
ANTIMALARIAL
ACTIVITY
OF
NOVEL
CLASS
OF
1,3-BENZOXABOROLE
DERIVATIVES
CONTAINING
1,3,4-OXADIAZOLE
MOIETY
285
VINAYAK
ADIMULE,
ADARSHA
HARAM
BALLI
JAGADEESHA
GOWDA,
SANTOSH
S,
NANDI,
AND
DEBDAS
BOWMIK
12.1
12.1.1
12.1.2
12.2
INTRODUCTION
285
MATERIALS
AND
METHODS
286
SYNTHESIS
287
EXPERIMENTAL
PROCEDURE
FOR
IN
VITRO
STUDIES
ON
ANTIMALARIAL
ACTIVITY
287
12.2.1
12.2.1.1
12.3
12.3.1
12.4
EXPERIMENTATION
289
ANALYTICAL
RESULTS
OF
THE
INTERMEDIATE
COMPOUNDS
(6A-10A)
289
ANALYTICAL
RESULTS
OF
INTERMEDIATE
COMPOUNDS
(12-16)
290
NMR
AND
CMR
ANALYSIS
290
SYNTHESIS
PROCEDURES
FOR
4-ETHOXY
PHENYL
BORONIC
ACID
(GENERAL
PROCEDURE
FOR
COMPOUNDS
2,3,
AND
4)
292
12.4.1
SYNTHESIS
OF
L-BROMO-4-(CYCLOPROPYL
METHYL)
BENZENE
(COMPOUND
2)
292
12.4.1.1
12.4.1.2
12.4.1.3
12.4.1.4
12.4.1.5
12.4.1.6
12.4.1.7
L-BROMO-4-(CYCLOPENTYL
METHOXY)BENZENE
(COMPOUND
2B)
292
L-BROMO-4-(CYCLOHEXYL
METHOXY)BENZENE
(COMPOUND
2C)
292
L-(BENZYLOXY)-4-BROMOBENZENE
(COMPOUND
2D)
293
L-BROMO-4-(PENTYLOXY)
BENZENE
(COMPOUND
2E)
293
SYNTHESIS
OF
4-METHOXY
PHENYL-BISPINACOLATO
ADDUCT
(3A)
293
SYNTHESIS
OF
4-METHOXY
PHENYL
BORONIC
ACID
293
GENERAL
PROCEDURE
FOR
THE
SYNTHESIS
OF
DERIVATIVES
(COMPOUNDS
6-10)
(STEP
II)
293
12.4.1.8
GENERAL
PROCEDURE
FOR
THE
SYNTHESIS
OF
DERIVATIVES
(COMPOUNDS
6A-10A)
293
12.4.1.9
GENERAL
PROCEDURE
FOR
THE
SYNTHESIS
OF
DERIVATIVES
(COMPOUNDS
12-16)
294
CONTENTS
XIII
12.5
12.5.1
12.6
RESULTS
AND
DISCUSSION
294
IN
VITRO
ANTIPLASMODIAL
ACTIVITY
294
CONCLUSION
297
AUTHORS
CONTRIBUTIONS
298
ACKNOWLEDGMENTS
298
CONFLICT
OF
INTEREST
298
REFERENCES
298
PART
IV
A
VACCINE
PERSPECTIVE
303
13
RECENT
ADVANCES
IN
MALARIA
VACCINE
DEVELOPMENT
305
SAILENDRA
KUMAR
MAHANTA
13.1
13.2
13.3
13.4
13.4.1
13.4.1.1
INTRODUCTION
305
HISTORY
OF
MALARIA
VACCINE
DEVELOPMENT
306
VACCINE
DESIGN
TARGETS
AND
APPROACHES
308
TYPES
OF
MALARIA
VACCINE
309
PRE-ERYTHROCYTIC
VACCINES
309
VACCINES
BASED
ON
THE
RTS,
-S,
AND
CSP
ENCODED
SECTIONS
OF
THE
MALARIA
GENE
310
13.4.2
13.4.3
13.4.4
13.4.5
13.4.6
13.5
WHOLE
SPOROZOITE
VACCINES
311
BLOOD
STAGE
VACCINES
(BSVS)
311
PLACENTAL
MALARIA
VACCINES
312
TRANSMISSION
BLOCKING
VACCINES
(TBV)
313
VACCINES
FOR
P.
VIVAX
314
CONCLUSIONS
314
REFERENCES
314
14
TOLL-LIKE
RECEPTOR-BASED
ADJUVANTS:
A
GATEWAY
TOWARD
IMPROVED
MALARIA
VACCINATION
319
DEEPIKA
KANNAN,
ARSHPREET
KAUR,
DEEPAK
B.
SALUNKE,
AND
SHAILJA
SINGH
14.1
14.2
14.2.1
14.2.2
14.3
14.3.1
14.3.2
14.3.3
14.4
INTRODUCTION
319
HOST
IMMUNOLOGICAL
RESPONSES
IN
MALARIA
CONFERRING
PROTECTION
322
INNATE
IMMUNITY
322
ADAPTIVE
IMMUNITY
324
CROSSTALK
OF
PRRS
IN
HOST
IMMUNE
SYSTEM
WITH
MALARIAL
ANTIGENS
326
GLYCOSYL
PHOSPHATIDYLINOSITOLS
(GPI)
328
PLASMODIAL
RNA
330
HEMOZOIN
(HZ)
330
SYNTHETIC
TLR
ADJUVANTS:
AN
APPROACH
TO
ENHANCE
VACCINE
IMMUNOGENICITY
331
14.4.1
14.4.2
14.4.3
14.4.4
TLR2
331
TLR4
333
TLR5
336
TLR7/8
337
XIV
CONTENTS
INDEX
367
14.4.5
14.5
TLR9
339
CONCLUSION
341
ABBREVIATIONS
341
REFERENCES
342
15
PURE
TLR7
AGONISTIC
BBIQ
IS
A
POTENTIAL
ADJUVANT
AGAINST
PLASMODIUM
BERGHEI
ANKA
CHALLENGE
IN
VIVO
353
RUCHIKA
SAROA,
DEEPENDER
KAUSHIK,
ARUNA
RAKHA,
UPMA
BAGAI,
SUKHBIR
KAUR,
AND
DEEPAK
B.
SALUNKE
15.1
15.2
15.2.1
15.2.2
15.2.3
15.2.4
15.2.5
15.3
15.4
15.5
15.6
15.7
15.8
15.9
15.10
15.10.1
15.10.2
15.10.3
15.10.4
15.10.5
15.11
INTRODUCTION
353
MATERIAL
AND
METHODS
354
EXPERIMENTAL
ANIMALS
354
ETHICAL
CLEARANCE
355
PARASITE
INFECTION
355
ISOLATION
OF
BLOOD
STAGE
FRACTION
355
ADJUVANT
355
IMMUNISATION
PROTOCOL
AND
POST-CHALLENGE
REGIME
356
STUDY
DESIGN
357
ISOLATION
OF
SPLENIC
LYMPHOCYTES
FROM
MICE
357
FACS
ANALYSIS
OF
ISOLATED
LYMPHOCYTES
357
IGGI
AND
IGG2A
ANTIBODY
RESPONSE
357
ESTIMATION
OF
VARIOUS
CYTOKINES
358
STATISTICAL
ANALYSIS
358
RESULTS
AND
DISCUSSION
358
COURSE
OF
INFECTION
358
FLOW
CYTOMETRIC
ANALYSIS
OF
SPLENIC
T
CELLS
AND
T
REG
CELLS
358
CYTOKINE
PROFILING
360
FLOW
CYTOMETRIC
ANALYSIS
OF
SPLENIC
B
CELLS
362
IGGI
AND
IGG2A
RESPONSE
362
CONCLUSION
363
CONFLICT
OF
INTERESTS
364
FUNDING
364
ACKNOWLEDGMENT
364
REFERENCES
364
|
| adam_txt |
CONTENTS
PART
1
INTRODUCTION
1
1
CHRONOLOGY
OF
DRUG
DEVELOPMENT
FOR
MALARIA
3
NALINI
KURUP
AND
NIKHIL
RAJNANI
1.1
1.1.1
1.2
1.2.1
1.3
1.3.1
1.4
1.4.1
1.5
1.6
1.6.1
1.7
1.7.1
INTRODUCTION
3
LIFE
CYCLE
OF
MALARIA
(ADAPTED
FROM
CDC)
4
MALARIA
-
ERSTWHILE
MEMORIES
5
PROGRESS
FIGHTING
MALARIA
5
CURRENT
CHEMOTHERAPY
USED
TO
TREAT
MALARIA
7
CURRENT
COMBINATION
THERAPY
13
DRUG
RESISTANCE
OF
ANTIMALARIAL
DRUGS
14
DETECTION
OF
DRUG
RESISTANCE
16
NEWER
DRUGS
APPROVED
FOR
MALARIA
TREATMENT
17
CURRENT
APPROACHES
TO
DEVELOPING
A
MALARIA
VACCINE
18
HOPE
FOR
VACCINE
LIES
IN
THE
PARASITE
ITSELF
18
CONCLUSION:
THE
PATH
FORWARD
20
RTS,
-S
VACCINE:
A
NEW
TOOL
WITH
POTENTIAL
FOR
AFRICA
20
REFERENCES
21
PART
II
CHALLENGES
AND
OPPORTUNITIES
IN
MALARIA
THERAPY
25
2
SCIENTIFIC
CHALLENGES
AND
TREATMENT
OPPORTUNITIES
IN
THE
FACE
OF
SHIFTING
MALARIA
EPIDEMIOLOGY
27
KETAKI
RAMANI
2.1
2.2
2.3
2.3.1
2.3.2
2.3.2.1
2.3.2.2
INTRODUCTION
27
THE
SCIENTIFIC
CHALLENGES
AGAINST
MALARIAL
DRUG
28
ADVANCES
IN
UNDERSTANDING
AND
MANAGING
DRUG
RESISTANCE
29
VECTOR
AND
ITS
CONTROL
29
PARASITE
AND
ITS
CONTROL
30
MALARIA
VACCINE
31
ANTIMALARIAL
DRUGS
31
VI
CONTENTS
2.4
2.4.1
2.4.2
2.5
2.6
METHODS
TO
ASSESS
THE
PRESENCE
AND
LEVEL
OF
DRUG
RESISTANCE
32
THERAPEUTIC
EFFICACY
OF
ANTIMALARIAL
DRUGS
32
MOLECULAR
MARKERS
ASSOCIATED
WITH
P.
FALCIPARUM
33
ANTIMALARIAL
DRUGS
CURRENTLY
IN
USE
AND
IN
THE
PIPELINE
33
FUTURE
38
REFERENCES
40
3
EMERGING
FORMULATION
TECHNOLOGIES
AGAINST
MALARIA
RESURGENCE
45
KINJAL
PARIKH,
RAKHEE
KAPADIA,
ROHAN
PAI,
MAHENDRA
PRAJAPATI,
AND
GANESH
SHEVALKAR
LIST
OF
ABBREVIATIONS
45
3.1
3.1.1
3.1.2
3.2
3.2.1
3.2.2
3.2.3
3.2.4
3.3
INTRODUCTION
46
MAJOR
PATHOLOGICAL
HALLMARKS
OF
MALARIA
46
CURRENT
TREATMENT
STRATEGIES
47
PITFALLS
OF
THE
CURRENT
TREATMENT
REGIMEN
47
DRUG
RESISTANCE
47
HIGH
DRUG
DOSE
48
LONG-TERM
TREATMENT
48
RECURRENCE
AND
REVERSION
OF
DISEASES
48
NANOTECHNOLOGY-BASED
STRATEGIES
FOR
TARGETING
IN
ANTIMALARIAL
THERAPY
49
3.3.1
3.3.2
3.3.2.1
3.3.2.2
3.3.2.3
3.3.3
3.4
3.4.1
3.4.1.1
3.4.1.2
3.4.1.3
PASSIVE
TARGETING
49
ACTIVE
TARGETING
49
HEPATOCYTE
TARGETING
50
ERYTHROCYTE
TARGETING
50
BRAIN
TARGETING
50
RAPID
DIAGNOSIS
AND
VECTOR
CONTROL
51
NANO
FORMULATIONS
FOR
MALARIAL
TREATMENT
51
LIPID-BASED
NANOPLATFORMS
52
NANOEMULSION
52
SELF-EMULSIFYING
DRUG
DELIVERY
SYSTEM
(SEDDS)
53
SOLID
LIPID
NANOPARTICLES
(SLNS)
AND
NANOSTRUCTURED
LIPID
CARRIERS
(NLCS)
54
3.4.1.4
3.4.2
3.4.2.1
3.4.2.2
3.4.2.3
3.4.2.4
3.4.2.5
3.4.2.6
3.4.3
3.4.4
3.4.4.1
LIPOSOME
54
POLYMER-BASED
NANOPLATFORMS
FOR
MALARIA
55
NANOPARTICLES
55
NANOCAPSULES
58
DENDRIMERS
58
MICELLES
59
POLYMERIC
HYDROGEL
NANOPARTICLES
59
NANOSUSPENSION
59
ORGANIZED
LAYER-BY-LAYER
ASSEMBLY
59
INORGANIC
NANO-ARCHITECTONICS
59
METALLIC
PLATFORMS
60
CONTENTS
VII
3.4.4.2
3.4.4.3
3.4.4.4
3.4.5
3.4.5.1
3.4.5.2
3.4.6
3.4.7
3.4.7.1
3.4.7.2
3.4.7.3
3.4.7.4
3.5
3.5.1
QUANTUM
DOTS
61
CARBON
NANOSTRUCTURES
62
BIO-CERAMICS
62
BIO-INSPIRED
NANOCARRIERS
63
VACCINES
BASED
ON
BIO-INSPIRED
NANOCARRIERS
63
BIO-ENGINEERED
STRATEGY
BASED
ON
ERYTHROCYTES
64
PROTEIN-PEPTIDE-BASED
DRUG
DELIVERY
SYSTEM
64
STIMULI-RESPONSIVE
PLATFORMS
FOR
MALARIA
64
PH-RESPONSIVE
FORMULATIONS
65
THERMO-RESPONSIVE
FORMULATIONS
65
REDOX
STATE
RESPONSIVE
SUBSTANCES
65
STIMULI-RESPONSIVE
LIQUID
CRYSTALLINE
MATERIALS
65
DIAGNOSTICS
66
STIMULI-RESPONSIVE
IRON
OXIDE
AND
GOLD
NANOPARTICLE
REAGENT
SYSTEM
66
3.5.2
3.5.3
3.6
3.6.1
3.6.2
3.6.3
3.6.4
IMMUNOLOGICAL
ADJUVANTS
66
NANOFIBERS
66
CHALLENGES
IN
CLINICAL
TRANSLATION
OF
NANOMEDICINE
67
BIOLOGICAL
CHALLENGES
67
BIOCOMPATIBILITY
AND
SAFETY
67
CHALLENGES
IN
MANUFACTURING
SCALE-UP
AND
REPRODUCIBILITY
67
ANALYTICAL
CHARACTERIZATION
AND
QUALITY
CONTROL
CHALLENGES
OF
NANO-FORMULATIONS
68
3.6.5
3.6.6
3.7
3.8
REGULATORY
CHALLENGES
68
OTHER
CHALLENGES
69
SUMMARY
AND
FUTURE
PERSPECTIVE
69
CONCLUSION
69
ACKNOWLEDGMENTS
70
REFERENCES
70
4
TARGETED
DRUG
DELIVERY
FOR
ANTIMALARIAL
THERAPY
83
SUHA
ZWAYEN,
TAMARA
ZWAIN,
AND
KAMALINDER
K.
SINGH
4.1
4.2
4.2.1
4.2.2
4.2.3
4.3
4.4
4.4.1
4.4.2
4.4.3
4.4.4
4.4.5
4.5
INTRODUCTION
83
REMODELLING
OF
PARASITE-INFECTED
RED
BLOOD
CELL
(PRBC)
84
THE
RED
BLOOD
CELL
MEMBRANE
(RBCM)
85
THE
PARASITOPHOROUS
VACUOLE
MEMBRANE
(PVM)
85
THE
PARASITE
PLASMA
MEMBRANE
(PPM)
86
THE
EMERGENCE
OF
RESISTANCE
AND
ANTIMALARIAL
THERAPY
APPROACH
86
NANOCARRIERS
FOR
ANTIMALARIAL
DRUG
DELIVERY
89
LIPOSOMES
89
SOLID
LIPID
NANOPARTICLES
(SLNS)
91
NANOSTRUCTURED
LIPID
CARRIERS
(NLCS)
91
NANO-EMULSIONS
(NES)
91
POLYMERIC
NANOPARTICLES
92
TARGETED
ANTIMALARIAL
DRUG
DELIVERY
SYSTEMS
92
VIII
CONTENTS
4.5.1
4.5.2
4.6
PASSIVE
DRUG
TARGETING
WITH
CONVENTIONAL
NANOCARRIERS
92
ACTIVE
DRUG
TARGETING
WITH
SURFACE-MODIFIED
NANOCARRIER
93
CONCLUSION:
MOVING
TOWARDS
THE
FUTURE
97
ACKNOWLEDGEMENTS
97
REFERENCES
97
5
THE
IMMINENT
THREAT
OF
ANTIMALARIAL
DRUG
RESISTANCE
105
BHARTI
SINGAL
AND
JYOTI
CHHIBBER-GOEL
5.1
5.2
5.3
5.3.1
5.3.2
5.3.3
5.3.4
5.4
5.4.1
5.4.2
5.4.3
5.4.3.1
5.4.3.2
5.4.4
5.4.4.1
5.4.4.2
5.5
5.5.1
5.5.2
5.5.3
5.6
INTRODUCTION
105
ANTIMALARIAL
DRUGS:
AN
OVERVIEW
107
THE
EVOLUTION
OF
CQ
RESISTANCE
109
MECHANISM
OF
ACTION
OF
CQ
109
BASIS
OF
CQ
RESISTANCE
110
PREVALENCE
OF
CQ
RESISTANCE
112
WHO
GUIDELINES
TO
USE
CQ
113
IMPACT
OF
SULFADOXINE-PYRIMETHAMINE
RESISTANCE
113
MECHANISM
OF
ACTION
OF
SP
114
SP
RESISTANCE
116
DISTRIBUTION
OF
DHPS
AND
DHFR
MUTATION
ACROSS
GLOBE
117
DHFR
117
DHPS
117
WHO
GUIDELINES
TO
USE
SP
118
IPTP
GUIDELINES
118
IPTI
GUIDELINES
118
ACT
RESISTANCE
118
MECHANISM
OF
ACTION
OF
ART
121
ART
RESISTANCE
AND
ACT
FAILURE
122
WHO
GUIDELINES
123
CONCLUSION:
THE
ROAD
AHEAD
124
REFERENCES
124
6
CURRENT
THERAPIES
AND
NEW
DRUG
TARGETS
FOR
THE
FUTURE
DRUG
DEVELOPMENT
OF
DRUG
RESISTANT
MALARIA
133
POOJA
MITTAL
AND
RUPESH
K.
GAUTAM
6.1
6.2
6.3
6.4
6.4.1
6.4.1.1
6.4.1.2
6.4.1.3
6.4.1.4
6.4.2
INTRODUCTION
133
LIFE
CYCLE
OF
PLASMODIUM
FALCIPARUM
134
CURRENT
ANTIMALARIAL
THERAPY
AND
THEIR
SHORTCOMINGS
134
DRUG
TARGETS
FOR
CURRENT
ANTIMALARIAL
THERAPY
136
DRUG-RESISTANT
MALARIA
AND
IDENTIFICATION
OF
NEW
TARGETS
137
FOOD
VACUOLE
AS
DRUG
TARGETS
137
SHIKIMIC
ACID
PATHWAY
TARGETING
142
TARGETING
FOLATE
PATHWAY
AND
METHIONINE
SYNTHESIS
PATHWAY
142
GLYCOLYTIC
PATHWAY
INHIBITION
144
MITOCHONDRIA
AS
DRUG
TARGETS
144
CONTENTS
IX
6.4.2.1
6.4.2.2
6.5
6.5.1
6.5.2
6.5.3
6.5.4
6.5.5
6.6
TARGETING
ELECTRON
TRANSPORT
CHAIN
144
INHIBITION
OF
DIHYDROORATE
DEHYDROGENASE
144
FUTURE
DRUG
DEVELOPMENT
FOR
THE
TREATMENT
OF
MALARIA
146
BENEFITS
OF
NANOCARRIERS
146
LIPID-BASED
DRUG
DELIVERY
146
LIPOSOMES (AS
NANOCARRIERS)
146
NANOSTRUCTURED
LIPID
CARRIERS
146
SOLID
LIPID
NANOCARRIERS
147
CONCLUSION
147
REFERENCES
147
PART
III
DRUG
DEVELOPMENT
151
7
ASSAYS
FOR
ANTIMALARIAL
DRUG
DISCOVERY
153
VARUN
GORKI,
NEHA
S.
WALTER,
AND
SUKHBIR
KAUR
7.1
7.2
7.2.1
7.2.2
7.2.3
7.2.4
INTRODUCTION
153
IN
VITRO
ASSAYS
FOR
ANTIMALARIAL
DRUG
DISCOVERY
155
SCHIZONT
MATURATION
INHIBITION
ASSAY
(MICROSCOPIC
TEST)
156
IN
VITRO
MICRO
TEST
TECHNIQUE
156
RADIOISOTOPE
ASSAY
156
COLORIMETRIC
ASSAY
(PLASMODIUM
LACTATE
DEHYDROGENASE
ASSAY
[PLDH])
157
7.2.5
7.2.5.1
7.2.5.2
7.2.6
7.2.7
7.2.8
7.2.9
7.2.10
7.2.11
ELISA-BASED
METHODS
157
DELI
ASSAY
157
ASSAY
BASED
ON
HISTIDINE-RICH
PROTEIN
II
(HRPII)
OF
P.
FALCIPARUM
158
FLOW
CYTOMETRY
158
FLUOROMETRIC
ASSAY
158
0-HEMATIN
FORMATION
(HAEMOZOIN
TEST)
159
DRUG
INTERACTION
ASSAY
AND
ISOBOLOGRAM
ANALYSIS
159
PCR-BASED
METHODS
160
IN
VITRO
ASSAYS
TARGETING EXO-ERYTHROCYTIC
AND
SEXUAL
STAGES
OF
THE
PARASITE
160
7.2.11.1
7.2.11.2
7.3
7.3.1
7.3.2
7.3.3
7.3.4
7.3.5
7.3.6
7.3.7
7.3.8
EXO-ERYTHROCYTIC
SCHIZONTOCIDAL
ASSAY
160
EX-FLAGELLATION
ASSAY
160
IN
VIVO
ASSAYS
FOR
ANTIMALARIAL
DRUG
DISCOVERY
161
PETERS
'
4-DAY
TEST
162
DOSE
RANGING
FULL
4-DAY
TEST
163
ONSET/RECRUDESCENCE
TEST
163
PREVENTIVE
TEST
166
CURATIVE
TEST
166
HILL
'
S
TEST
FOR
CAUSAL
PROPHYLAXIS
AND
RESIDUAL
ACTIVITY
166
ASSAYS
WITH
P.
BERGHEI
GREEN
FLUORESCENT
PROTEIN
(PBGFP)
167
ASSAYS
EMPLOYING
IMMUNOCOMPROMISED
MICE
167
X
CONTENTS
7.3.9
7.3.10
7.3.11
7.4
7.5
7.5.1
7.5.2
7.5.3
7.5.4
7.5.5
7.6
7.6.1
7.6.1.1
7.6.1.2
7.6.2
7.7
PRIMATE
MODELS
FOR
IN
VIVO
STUDIES
168
SPORONTOCIDAL
ASSAYS
169
ANTI-SPOROZOITE
ASSAY
169
EX
VIVO
ASSAYS
FOR
ANTIMALARIAL
DRUG
DISCOVERY
169
ASSAYS
FOR
ASSESSMENT
OF
IN
VITRO
TOXICITY
170
MTT
ASSAY
170
XTT
ASSAY
172
LDH
(LACTATE
DEHYDROGENASE)
ASSAY
172
PROTEIN
CONTENT
ASSAY
173
NEUTRAL
RED
UPTAKE
ASSAY
(NRU)
173
ASSAYS
FOR
ASSESSMENT
OF
IN
VIVO
TOXICITY
173
ACUTE
TOXICITY
174
LIMIT
TEST
OF
LORKE
175
UP
AND
DOWN
PROCEDURE
175
CHRONIC
TOXICITY
175
CONCLUSION
176
REFERENCES
177
8
AMINOACYL-TRNA
SYNTHETASES
AS
MALARIAL
DRUG
TARGETS:
A
STRUCTURAL
BIOLOGY
PERSPECTIVE
187
BHARTI
SINGAL
AND
JYOTI
CHHIBBER-GOEL
8.1
8.2
8.2.1
8.2.2
8.3
8.4
8.4.1
8.4.2
8.4.3
8.4.4
8.5
8.5.1
8.5.2
8.6
8.6.1
8.7
8.7.1
8.7.2
8.8
8.9
INTRODUCTION
187
PF/PV^BES
188
PF/PV
GENOME
188
AMINOACYL-TRNA
SYNTHETASES
(AARSS)
189
AMINOACYL-TRNA
SYNTHETASES
AS
DRUGGABLE
TARGETS
190
BIOCHEMICAL
SCREENING
OF
DRUG
LIBRARIES
192
COLORIMETRIC
ASSAYS
192
ENZYME
COUPLED
ASSAYS
193
LUCIFERASE
ASSAY
193
ASSAY
TO
TEST
SYNTHETIC
AS
WELL
AS
PROOFREADING
ACTIVITY
193
STRUCTURALLY
VALIDATED
PF/PV-AARSS
AS
DRUG
TARGETS
194
LYSYL-TRNA
SYNTHETASE
(KRS)
194
PROLYL-TRNA
SYNTHETASE
197
POTENTIAL
DRUG
TARGETS
PF/PV-AARSS
199
LEUCYL-TRNA
SYNTHETASE
(LRS)
199
ARGINYL-TRNA
SYNTHETASE
(RRS)
199
TRYPTOPHANYL-TRNA
SYNTHETASE
(WRS)
201
TYROSYL-TRNA
SYNTHETASE
202
OTHERS
203
CONCLUSION:
THE
ROAD
AHEAD
203
REFERENCES
204
CONTENTS
|
XI
9
NATURAL
PRODUCTS
AS
A
SOURCE
FOR
ANTIMALARIAL
DRUG
DEVELOPMENT
PROCESS
-
AN
OVERVIEW
213
UMA
R.
LAL
AND
SNIGDHA
LAL
9.1
INTRODUCTION
213
9.2
PHYTOCHEMICALS
AS
ANTIMALARIAL
AGENTS:
RECENT
DEVELOPMENTS
214
9.2.1
ALKALOIDS
214
9.2.2
TERPENES
219
9.2.2.1
SESQUITERPENE
LACTONES
219
9.2.2.2
DITERPENES
220
9.2.2.3
TRITERPENES
222
9.2.2.4
STEROIDS
AND
OTHERS
224
9.2.3
POLYPHENOLS
224
9.2.3.1
BIFLAVONOIDS
224
9.2.3.2
PRENYLATED
FLAVONOIDS
226
9.2.3.3
OTHER
FLAVONOIDS
226
9.3
TRADITIONAL
SYSTEM
OF
MEDICINE
AND
MALARIA
227
9.3.1
PLANTS/FORMULATIONS
USED
IN
MALARIA
TREATMENT
IN
AYURVEDIC
SYSTEM
OF
MEDICINE
227
9.4
CONCLUSIONS
228
REFERENCES
228
10
MUSHROOM-DERIVED
PRODUCTS
AS
AN
ALTERNATIVE
ANTIMALARIAL
THERAPEUTICS:
A
REVIEW
235
SENZOSENKOSI
S.
MKHIZE,
KGOTHATSO
E.
MACHABA,
MTHOKOZISI
B.
C.
SIMELANE,
AND
OFENTSE
J.
POOE
10.1
INTRODUCTION
235
10.2
BIOLOGICAL
ROLES
OF
MUSHROOMS
235
10.2.1
MALARIAL
HISTORY
AND
IMPACT
235
10.2.2
ANTIMALARIAL
ACTIVITY
OF
MUSHROOM
EXTRACTS
237
10.2.3
BIOACTIVE
MOLECULES
FOUND
WITHIN
MUSHROOMS
239
10.2.4
PHYTOCHEMICAL
PROPERTIES
OF
MUSHROOM
DERIVED
ANTIMALARIAL
PRODUCTS
241
10.2.5
IMMUNOMODULATORY
PROPERTIES
OF
MUSHROOMS
243
10.3
CONCLUSION
243
ACKNOWLEDGEMENTS
244
REFERENCES
244
11
DISCOVERY
AND
TRENDS
OF
8-AMINOQUINOLINE
AND
4-AMINOQUINOLINE
CLASSES
OF
ANTIMALARIALS
251
MEENAKSHI
JAIN,
SAMARPITA
DAS,
AND
RAHUL
JAIN
11.1
INTRODUCTION
251
11.1.1
HISTORY
251
XII
CONTENTS
11.1.2
11.1.3
11.1.3.1
11.1.3.2
11.2
MODE
OF
ACTION
253
SAR
OF
AMINOQUINOLINES
255
SAR
OF
8-AMINOQUINOLINES
255
SAR
OF
4
AMINOQUINOLINES
257
SYNTHETIC
APPROACHES
OF
8-AMINOQUINOLINES
AND
4-AMINOQUINOLINES
259
11.2.1
11.2.1.1
11.2.1.2
11.2.2
11.2.2.1
11.2.2.2
11.3
SYNTHETIC
APPROACH
OF
8-AMINOQUINOLINES
259
SYNTHETIC
APPROACH
OF
WELL-ESTABLISHED
DRUGS
259
SYNTHETIC
APPROACH
OF
RECENTLY
DEVELOPED
PQ
CONGENERS
269
SYNTHETIC
APPROACHES
OF
4-AMINOQUINOLINES
270
SYNTHETIC
APPROACHES
TO
WELL-ESTABLISHED
DRUGS
270
SYNTHETIC
APPROACH
OF
PQ-CQ
HYBRID
280
CONCLUSION
AND
FUTURE
PERSPECTIVES
280
ACKNOWLEDGMENT
281
REFERENCES
281
12
ANTIMALARIAL
ACTIVITY
OF
NOVEL
CLASS
OF
1,3-BENZOXABOROLE
DERIVATIVES
CONTAINING
1,3,4-OXADIAZOLE
MOIETY
285
VINAYAK
ADIMULE,
ADARSHA
HARAM
BALLI
JAGADEESHA
GOWDA,
SANTOSH
S,
NANDI,
AND
DEBDAS
BOWMIK
12.1
12.1.1
12.1.2
12.2
INTRODUCTION
285
MATERIALS
AND
METHODS
286
SYNTHESIS
287
EXPERIMENTAL
PROCEDURE
FOR
IN
VITRO
STUDIES
ON
ANTIMALARIAL
ACTIVITY
287
12.2.1
12.2.1.1
12.3
12.3.1
12.4
EXPERIMENTATION
289
ANALYTICAL
RESULTS
OF
THE
INTERMEDIATE
COMPOUNDS
(6A-10A)
289
ANALYTICAL
RESULTS
OF
INTERMEDIATE
COMPOUNDS
(12-16)
290
NMR
AND
CMR
ANALYSIS
290
SYNTHESIS
PROCEDURES
FOR
4-ETHOXY
PHENYL
BORONIC
ACID
(GENERAL
PROCEDURE
FOR
COMPOUNDS
2,3,
AND
4)
292
12.4.1
SYNTHESIS
OF
L-BROMO-4-(CYCLOPROPYL
METHYL)
BENZENE
(COMPOUND
2)
292
12.4.1.1
12.4.1.2
12.4.1.3
12.4.1.4
12.4.1.5
12.4.1.6
12.4.1.7
L-BROMO-4-(CYCLOPENTYL
METHOXY)BENZENE
(COMPOUND
2B)
292
L-BROMO-4-(CYCLOHEXYL
METHOXY)BENZENE
(COMPOUND
2C)
292
L-(BENZYLOXY)-4-BROMOBENZENE
(COMPOUND
2D)
293
L-BROMO-4-(PENTYLOXY)
BENZENE
(COMPOUND
2E)
293
SYNTHESIS
OF
4-METHOXY
PHENYL-BISPINACOLATO
ADDUCT
(3A)
293
SYNTHESIS
OF
4-METHOXY
PHENYL
BORONIC
ACID
293
GENERAL
PROCEDURE
FOR
THE
SYNTHESIS
OF
DERIVATIVES
(COMPOUNDS
6-10)
(STEP
II)
293
12.4.1.8
GENERAL
PROCEDURE
FOR
THE
SYNTHESIS
OF
DERIVATIVES
(COMPOUNDS
6A-10A)
293
12.4.1.9
GENERAL
PROCEDURE
FOR
THE
SYNTHESIS
OF
DERIVATIVES
(COMPOUNDS
12-16)
294
CONTENTS
XIII
12.5
12.5.1
12.6
RESULTS
AND
DISCUSSION
294
IN
VITRO
ANTIPLASMODIAL
ACTIVITY
294
CONCLUSION
297
AUTHORS
CONTRIBUTIONS
298
ACKNOWLEDGMENTS
298
CONFLICT
OF
INTEREST
298
REFERENCES
298
PART
IV
A
VACCINE
PERSPECTIVE
303
13
RECENT
ADVANCES
IN
MALARIA
VACCINE
DEVELOPMENT
305
SAILENDRA
KUMAR
MAHANTA
13.1
13.2
13.3
13.4
13.4.1
13.4.1.1
INTRODUCTION
305
HISTORY
OF
MALARIA
VACCINE
DEVELOPMENT
306
VACCINE
DESIGN
TARGETS
AND
APPROACHES
308
TYPES
OF
MALARIA
VACCINE
309
PRE-ERYTHROCYTIC
VACCINES
309
VACCINES
BASED
ON
THE
RTS,
-S,
AND
CSP
ENCODED
SECTIONS
OF
THE
MALARIA
GENE
310
13.4.2
13.4.3
13.4.4
13.4.5
13.4.6
13.5
WHOLE
SPOROZOITE
VACCINES
311
BLOOD
STAGE
VACCINES
(BSVS)
311
PLACENTAL
MALARIA
VACCINES
312
TRANSMISSION
BLOCKING
VACCINES
(TBV)
313
VACCINES
FOR
P.
VIVAX
314
CONCLUSIONS
314
REFERENCES
314
14
TOLL-LIKE
RECEPTOR-BASED
ADJUVANTS:
A
GATEWAY
TOWARD
IMPROVED
MALARIA
VACCINATION
319
DEEPIKA
KANNAN,
ARSHPREET
KAUR,
DEEPAK
B.
SALUNKE,
AND
SHAILJA
SINGH
14.1
14.2
14.2.1
14.2.2
14.3
14.3.1
14.3.2
14.3.3
14.4
INTRODUCTION
319
HOST
IMMUNOLOGICAL
RESPONSES
IN
MALARIA
CONFERRING
PROTECTION
322
INNATE
IMMUNITY
322
ADAPTIVE
IMMUNITY
324
CROSSTALK
OF
PRRS
IN
HOST
IMMUNE
SYSTEM
WITH
MALARIAL
ANTIGENS
326
GLYCOSYL
PHOSPHATIDYLINOSITOLS
(GPI)
328
PLASMODIAL
RNA
330
HEMOZOIN
(HZ)
330
SYNTHETIC
TLR
ADJUVANTS:
AN
APPROACH
TO
ENHANCE
VACCINE
IMMUNOGENICITY
331
14.4.1
14.4.2
14.4.3
14.4.4
TLR2
331
TLR4
333
TLR5
336
TLR7/8
337
XIV
CONTENTS
INDEX
367
14.4.5
14.5
TLR9
339
CONCLUSION
341
ABBREVIATIONS
341
REFERENCES
342
15
PURE
TLR7
AGONISTIC
BBIQ
IS
A
POTENTIAL
ADJUVANT
AGAINST
PLASMODIUM
BERGHEI
ANKA
CHALLENGE
IN
VIVO
353
RUCHIKA
SAROA,
DEEPENDER
KAUSHIK,
ARUNA
RAKHA,
UPMA
BAGAI,
SUKHBIR
KAUR,
AND
DEEPAK
B.
SALUNKE
15.1
15.2
15.2.1
15.2.2
15.2.3
15.2.4
15.2.5
15.3
15.4
15.5
15.6
15.7
15.8
15.9
15.10
15.10.1
15.10.2
15.10.3
15.10.4
15.10.5
15.11
INTRODUCTION
353
MATERIAL
AND
METHODS
354
EXPERIMENTAL
ANIMALS
354
ETHICAL
CLEARANCE
355
PARASITE
INFECTION
355
ISOLATION
OF
BLOOD
STAGE
FRACTION
355
ADJUVANT
355
IMMUNISATION
PROTOCOL
AND
POST-CHALLENGE
REGIME
356
STUDY
DESIGN
357
ISOLATION
OF
SPLENIC
LYMPHOCYTES
FROM
MICE
357
FACS
ANALYSIS
OF
ISOLATED
LYMPHOCYTES
357
IGGI
AND
IGG2A
ANTIBODY
RESPONSE
357
ESTIMATION
OF
VARIOUS
CYTOKINES
358
STATISTICAL
ANALYSIS
358
RESULTS
AND
DISCUSSION
358
COURSE
OF
INFECTION
358
FLOW
CYTOMETRIC
ANALYSIS
OF
SPLENIC
T
CELLS
AND
T
REG
CELLS
358
CYTOKINE
PROFILING
360
FLOW
CYTOMETRIC
ANALYSIS
OF
SPLENIC
B
CELLS
362
IGGI
AND
IGG2A
RESPONSE
362
CONCLUSION
363
CONFLICT
OF
INTERESTS
364
FUNDING
364
ACKNOWLEDGMENT
364
REFERENCES
364 |
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| genre | (DE-588)4143413-4 Aufsatzsammlung gnd-content |
| genre_facet | Aufsatzsammlung |
| id | DE-604.BV047958174 |
| illustrated | Illustrated |
| index_date | 2024-07-03T19:39:41Z |
| indexdate | 2024-07-10T09:26:44Z |
| institution | BVB |
| isbn | 9783527348602 |
| language | English |
| oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-033339420 |
| oclc_num | 1355305612 |
| open_access_boolean | |
| owner | DE-11 |
| owner_facet | DE-11 |
| physical | xiv, 378 Seiten Illustrationen, Diagramme |
| publishDate | 2023 |
| publishDateSearch | 2023 |
| publishDateSort | 2023 |
| publisher | Wiley-VCH |
| record_format | marc |
| spelling | Drug development for Malaria novel approaches for prevention and treatment edites by Pravin Kendrekar Weinheim Wiley-VCH [2023] xiv, 378 Seiten Illustrationen, Diagramme txt rdacontent n rdamedia nc rdacarrier Arzneimittelentwicklung (DE-588)4143176-5 gnd rswk-swf Antimalariamittel (DE-588)4142684-8 gnd rswk-swf Biowissenschaften Chemie Chemistry Drug Discovery & Development Infectious Disease Infektionskrankheiten Life Sciences Medical Science Medizin Parasitologie Parasitology Wirkstoffforschung u. -entwicklung CH61: Wirkstoffforschung u. -entwicklung LSE0: Parasitologie MDD2: Infektionskrankheiten (DE-588)4143413-4 Aufsatzsammlung gnd-content Antimalariamittel (DE-588)4142684-8 s Arzneimittelentwicklung (DE-588)4143176-5 s DE-604 Kendrekar, Pravin (DE-588)1271144336 edt Erscheint auch als Online-Ausgabe, PDF 978-3-527-83060-2 Erscheint auch als Online-Ausgabe, EPUB 978-3-527-83059-6 Erscheint auch als Online-Ausgabe, oBook 978-3-527-83058-9 DNB Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=033339420&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis 1\p vlb 20210917 DE-101 https://d-nb.info/provenance/plan#vlb |
| spellingShingle | Drug development for Malaria novel approaches for prevention and treatment Arzneimittelentwicklung (DE-588)4143176-5 gnd Antimalariamittel (DE-588)4142684-8 gnd |
| subject_GND | (DE-588)4143176-5 (DE-588)4142684-8 (DE-588)4143413-4 |
| title | Drug development for Malaria novel approaches for prevention and treatment |
| title_auth | Drug development for Malaria novel approaches for prevention and treatment |
| title_exact_search | Drug development for Malaria novel approaches for prevention and treatment |
| title_exact_search_txtP | Drug development for Malaria novel approaches for prevention and treatment |
| title_full | Drug development for Malaria novel approaches for prevention and treatment edites by Pravin Kendrekar |
| title_fullStr | Drug development for Malaria novel approaches for prevention and treatment edites by Pravin Kendrekar |
| title_full_unstemmed | Drug development for Malaria novel approaches for prevention and treatment edites by Pravin Kendrekar |
| title_short | Drug development for Malaria |
| title_sort | drug development for malaria novel approaches for prevention and treatment |
| title_sub | novel approaches for prevention and treatment |
| topic | Arzneimittelentwicklung (DE-588)4143176-5 gnd Antimalariamittel (DE-588)4142684-8 gnd |
| topic_facet | Arzneimittelentwicklung Antimalariamittel Aufsatzsammlung |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=033339420&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
| work_keys_str_mv | AT kendrekarpravin drugdevelopmentformalarianovelapproachesforpreventionandtreatment |