| Autor: |
Sheppard GS; Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois 60064., Pireh D, Carrera GM Jr, Bures MG, Heyman HR, Steinman DH, Davidsen SK, Phillips JG, Guinn DE, May PD, et. al. |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 1994 Jun 24; Vol. 37 (13), pp. 2011-32. |
| DOI: |
10.1021/jm00039a015 |
| Abstrakt: |
(2RS,4R)-3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles represent a new class of potent, orally active antagonists of platelet activating factor (PAF). The compounds were prepared by acylation of the magnesium or zinc salts of substituted indoles with (2RS,4R)-2-(3-pyridinyl)-3-(tert-butoxycarbonyl)thiazolidin-4-oyl chloride. The 3-acylindole moiety functions as a hydrolytically stabilized and conformationally restricted anilide replacement, which imparts a considerable boost in potency to the series. Structure-activity relationships observed for substitution on the indole ring system are discussed. Members of the series compare favorably with other reported PAF antagonists. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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