Development of a series of phenyltetrazole leukotriene D4(LTD4) receptor antagonists
| Autor: | David K. Herron, Bollinger Ng, Baldwin Rf, Jason Scott Sawyer, Carlos R. Roman, Richard Waltz Harper, L E Rinkema, Jerome H. Fleisch |
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| Rok vydání: | 1992 |
| Předmět: |
Male
Models Molecular Receptors Leukotriene LTD4 receptor Leukotriene D4 Molecular Structure Molecular model Protein Conformation Chemistry Stereochemistry Guinea Pigs Antagonist Tetrazoles respiratory system Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Eicosanoid Ileum Drug Discovery Animals Molecular Medicine Moiety lipids (amino acids peptides and proteins) Receptors Immunologic |
| Zdroj: | Journal of Medicinal Chemistry. 35:1191-1200 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | A hypothetical model for receptor binding of leukotriene D4 (LTD4) was deduced from conformational analysis of LTD4 and from the structure-activity relationships (SAR) of known LTD4 receptor antagonists. A new structural series of LTD4 receptor antagonists exemplified by 5-[4-(4-phenylbutoxy)phenyl]-2-[4-(tetrazol-5-yl)butyl]-2H-t etrazole was designed in which a phenyltetrazole moiety was incorporated as a receptor binding equivalent of the triene unit of LTD4. A number of these phenyltetrazoles were prepared and found to possess LTD4 receptor antagonist activity. The structure-activity relationship (SAR) of this series is described. |
| Databáze: | OpenAIRE |
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