Azabicyclic indole esters as potent 5-HT4 receptor antagonists.
作者信息
Wyman P A, Gaster L M, King F D, Sutton J M, Ellis E S, Wardle K A, Young T J
机构信息
SmithKline Beecham Pharmaceuticals, Harlow, Essex, U.K.
出版信息
Bioorg Med Chem. 1996 Feb;4(2):255-61. doi: 10.1016/0968-0896(96)00037-5.
PMID:8814883
Abstract
The synthesis of a series of azabicyclic indole esters is described and their potency reported as 5-HT4 receptor antagonists. Optimization of the most potent compound (19) by preparing the corresponding oxazino[3,2-a]indole ester afforded 34, which had a pIC50 of 9.5 in the guinea pig distal colon longitudinal muscle myenteric plexus preparation.
摘要
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