Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX:
Gespeichert in:
| 1. Verfasser: | |
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| Format: | Abschlussarbeit Buch |
| Sprache: | English |
| Veröffentlicht: |
2013
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| Schlagworte: | |
| Online-Zugang: | Inhaltsverzeichnis |
| Beschreibung: | 176 S. graph. Darst. |
Internformat
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Datensatz im Suchindex
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INDEX
1 INTRODUCTION 1
1.1 BACKGROUND 4
1.1.1 EICOSANOIDS 4
1.1.2 ARACHIDONIC ACID 7
1.1.3 THE CYCLOOXYGENASE PATHWAY 9
1.1.4 BIOSYNTHESIS OF PROSTANOIDS 12
1.2 NON-STEROIDAL ANTI-INFLAMMATORY DRUGS 17
1.3 NON-SELECTIVE NSAIDS 18
1.4 COX-2 SELECTIVE NSAIDS 20
1.4.1 ROLES OF COX-1 AND COX-2 IN KIDNEY FUNCTION 21
1.4.2 ROLES OF COX-1 AND COX-2 IN THE CARDIOVASCULAR SYSTEM 23
1.5 MICROSOMAL PROSTAGLANDIN E SYNTHASE-1 25
1.5.1 ROLE OF MPGES-1 IN ARTHRITIS, FEVER, AND PAIN 27
1.5.2 ROLE OF MPGES-1 IN CARDIOVASCULAR DISEASES 29
1.5.3 ROLE OF MPGES-1 IN CARCINOGENESIS 31
1.5.4 ROLE OF MPGES-1 IN FACILITATION OF ANGIOGENESIS AND THE HEALING OF
GASTRIC ULCERS 34
1.5.5 ROLE OF MPGES-1 IN ALZHEIMER'S DISEASE 35
1.5.6 MICROSOMAL PROSTAGLANDIN E SYNTHASE-1 INHIBITORS 36
2 OBJECTIVE 39
3 CHEMISTRY 40
HTTP://D-NB.INFO/1047206463
3.1 SYNTHESIS OF COUPLED NSALDS WITH SULFON-AMIDES 41
3.2 MODIFYING LONAZOLAC DERIVATIVE BY SUZUKI COUPLING 43
3.3 ULLMAN CONDENSATION 44
3.4 SYNTHESIS OF INDOMETHACIN DERIVATIVES 45
3.4.1 FISHER INDOLE SYNTHESIS 46
3.4.2 SYNTHESIS OF COMPOUNDS 16 TO 19 48
3.4.3 COPPER-FREE SONOGASHIRA CROSS COUPLING 49
3.4.4 COUPLING CARBOXYLIC ACIDS WITH SULFONAMIDES SO
3.5 SYNTHESIS OF LONAZOLAC DERIVATIVES 52
3.5.1 HYDRAZONE SYNTHESIS 53
3.5.2 SYNTHESIS OF FORMYL PYRAZOLES USING VILSMEIER HAACK REACTION 53
3.5.3 OXIDATION AND REDUCTION OF FORMYLATED PYRAZOLES 56
3.5.4 WITTIG REACTION 56
3.5.5 CONVERSION OF ALCOHOLS TO CHLORIDES WITH SOCB 58
3.5.6 ACIDIC HYDROLYSIS OF NITRILES 58
3.5.7 COPPER-FREE SONOGASHIRA CROSS COUPLING 60
3.5.8 COUPLING CARBOXYLIC ACIDS WITH SULFONAMIDES 61
3.5.9 COUPLING CARBOXYLIC ACIDS WITH PHOSPHATES 62
4 BIOLOGICAL EVALUATION 63
4.1 MPGES-1 ASSAY
170
63
4.2 5-LOX ASSAY 64
4.2.1 ISOLATION OF NEUTROPHILS
173
'
171
64
4.2.2 DETERMINATION OF 5-LOX PRODUCT FORMATION IN NEUTROPHILS 64
4.3 COX-1 ASSAY
171
65
4.4 RESULTS AND DISCUSSION 66
4.4.1 INDOMETHACIN DERIVATIVES AS DUAL INHIBITORS OF MPGES-1 AND S-LOX
70
4.4.2 LONAZOLAC DERIVATIVES AS DUAL INHIBITORS OF MPGES-1 AND 5-LOX .73
5 CONCLUSION 78
6 EXPERIMENTAL 79
6.1 METHODS AND INSTRUMENTS 79
6.2 SYNTHETIC PROCEDURES 83
7 REFERENCES 161 |
| any_adam_object | 1 |
| author | Elkady, Mahmoud Ahmed Mohamed Moustafa |
| author_GND | (DE-588)1046085727 |
| author_facet | Elkady, Mahmoud Ahmed Mohamed Moustafa |
| author_role | aut |
| author_sort | Elkady, Mahmoud Ahmed Mohamed Moustafa |
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| bvnumber | BV041698354 |
| ctrlnum | (OCoLC)877993349 (DE-599)BSZ399373322 |
| dewey-full | 610 540 |
| dewey-hundreds | 600 - Technology (Applied sciences) 500 - Natural sciences and mathematics |
| dewey-ones | 610 - Medicine and health 540 - Chemistry and allied sciences |
| dewey-raw | 610 540 |
| dewey-search | 610 540 |
| dewey-sort | 3610 |
| dewey-tens | 610 - Medicine and health 540 - Chemistry and allied sciences |
| discipline | Chemie / Pharmazie Medizin |
| format | Thesis Book |
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| illustrated | Illustrated |
| indexdate | 2024-10-10T14:00:29Z |
| institution | BVB |
| language | English |
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| spelling | Elkady, Mahmoud Ahmed Mohamed Moustafa Verfasser (DE-588)1046085727 aut Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX vorgelegt von Mahmoud Ahmed Mohamed Moustafa Elkady 2013 176 S. graph. Darst. txt rdacontent n rdamedia nc rdacarrier Tübingen, Univ., Diss., 2013 Nichtsteroidales Antiphlogistikum (DE-588)4209813-0 gnd rswk-swf Inhibitor (DE-588)4027007-5 gnd rswk-swf Lipoxygenase 5- (DE-588)4285886-0 gnd rswk-swf (DE-588)4113937-9 Hochschulschrift gnd-content Lipoxygenase 5- (DE-588)4285886-0 s Inhibitor (DE-588)4027007-5 s Nichtsteroidales Antiphlogistikum (DE-588)4209813-0 s DE-604 DNB Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=027138730&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Elkady, Mahmoud Ahmed Mohamed Moustafa Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX Nichtsteroidales Antiphlogistikum (DE-588)4209813-0 gnd Inhibitor (DE-588)4027007-5 gnd Lipoxygenase 5- (DE-588)4285886-0 gnd |
| subject_GND | (DE-588)4209813-0 (DE-588)4027007-5 (DE-588)4285886-0 (DE-588)4113937-9 |
| title | Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX |
| title_auth | Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX |
| title_exact_search | Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX |
| title_full | Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX vorgelegt von Mahmoud Ahmed Mohamed Moustafa Elkady |
| title_fullStr | Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX vorgelegt von Mahmoud Ahmed Mohamed Moustafa Elkady |
| title_full_unstemmed | Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX vorgelegt von Mahmoud Ahmed Mohamed Moustafa Elkady |
| title_short | Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX |
| title_sort | modified acidic nonsteroidal anti inflammatory drugs as dual inhibitors of mpges 1 and 5 lox |
| topic | Nichtsteroidales Antiphlogistikum (DE-588)4209813-0 gnd Inhibitor (DE-588)4027007-5 gnd Lipoxygenase 5- (DE-588)4285886-0 gnd |
| topic_facet | Nichtsteroidales Antiphlogistikum Inhibitor Lipoxygenase 5- Hochschulschrift |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=027138730&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
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