DUAL ANTAGONISTS OF PLATELET-ACTIVATING-FACTOR AND HISTAMINE .2. PYRIDINE RING SUBSTITUTION OF N-ACETYL-4-(8-CHLORO-5,6-DIHYDRO-11H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIDIN-11-YLIDENE)PIPERIDINES

被引:17
作者
WONG, JK [1 ]
PIWINSKI, JJ [1 ]
GREEN, MJ [1 ]
GANGULY, AK [1 ]
ANTHES, JC [1 ]
BILLAH, MM [1 ]
机构
[1] SCHERING PLOUGH RES INST, DEPT ALLERGY & IMMUNOL, KENILWORTH, NJ 07033 USA
关键词
D O I
10.1016/S0960-894X(00)80290-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of pyridine ring substituted 1-acetyl-4-(8-chloro-5,6-dihydro-11H-benzo[5,6] cyclohepta[1,2-b]pyridin-11-ylidene)piperidines which are antagonists of both PAF and histamine were prepared by one of three different methods. Analogs with substitutents at C-3 were found to be the best dual antagonists among their corresponding regioisomers. Analogs with an electron donating substituent at the C-3 position are generally better antagonists of both PAF and histamine than analogs with electron withdrawing groups.
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页码:1073 / 1078
页数:6
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