CYCLIC ETHER ACETAL PLATELET-ACTIVATING-FACTOR (PAF) RECEPTOR ANTAGONISTS .2. IMIDAZO[4,5-C]PYRIDYL DERIVATIVES

Authors
WOOD LM WHITTAKER M TIMMIS DJ THOMPSON TM SAROGLOU L MILLER A DAVIDSON AH CHRISTODOULOU MS CACKETT KS BOWLES SA BEBBINGTON DS
Citation
Lm. Wood et al., CYCLIC ETHER ACETAL PLATELET-ACTIVATING-FACTOR (PAF) RECEPTOR ANTAGONISTS .2. IMIDAZO[4,5-C]PYRIDYL DERIVATIVES, Bioorganic & medicinal chemistry letters, 3(8), 1993, pp. 1499-1504
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
8
Year of publication
1993
Pages
1499 - 1504
Database
ISI
SICI code
0960-894X(1993)3:8<1499:CEAP(R>2.0.ZU;2-G
Abstract
The 1H-2-methylimidazo[4,5-c]pyridyl group has been found to be the op timal heterocycle for a series of cyclic ether acetal PAF antagonists. A lead compound 8 inhibits [H-3]-PAF receptor binding to washed human platelets with an IC50 value of 15 nM, and both PAF-induced hypotensi on and endotoxin-induced hypotension in anaesthetised rats with ED50 v alues of 1.4 mug/kg i.v. and 19 mug/kg i.v. respectively.