CONFORMATIONALLY-RESTRICTED ANALOGS OF TXA2 ANTAGONIST SQ-33961 - RECEPTOR-BINDING CONFORMATION OF THE CARBOXYL SIDE-CHAIN

被引：2
|
作者：
MISRA, RN
BROWN, BR
HARRIS, DN
PUDZIANOWSKI, AT
机构：
[1] Bristol-Myers Squibb, Pharmaceutical Research Institute, Princeton, NJ 08543-4000
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1991年 / 1卷 / 09期
关键词：
D O I：
10.1016/S0960-894X(01)81107-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two distinct conformational families, exemplified by 1 and 2, of thromboxane A2 (TxA2) receptor antagonist SQ 33,961 have been determined by molecular modeling. Synthesis and biological evaluation of conformationally-restricted mimic 3Z suggested that the hairpin conformer, 1, is the bioactive conformation.
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页码：465 / 470
页数：6
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