A NOVEL AND SELECTIVE CLASS OF AZABICYCLIC MUSCARINIC AGONISTS INCORPORATING AN N-METHOXY IMIDOYL HALIDE OR NITRILE FUNCTIONALITY

被引：17

作者：

BROMIDGE, SM

BROWN, F

CASSIDY, F

CLARK, MSG

DABBS, S

HAWKINS, J

LOUDON, JM

ORLEK, BS

RILEY, GJ

机构：

[1] SmithKline Beecham Pharmaceuticals, Harlow, Essex CM19 5AD, Medicinal Research Centre Coldharbour Road, Pinnacles

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)80533-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structural modulation of the oxime ether group of a series of azabicyclic oxime ethers by the incorporation of electron-withdrawing groups has led to a novel class of N-methoxy imidoyl halides and nitriles which are potent muscarinic agonists. Members of this class, exemplified by 2e and 3c, show favourable central selectivity which can be rationalised in terms of partial agonist character, improved physicochemical properties, and receptor sub-type selectivity.

引用

页码：791 / 796

页数：6

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