SYNTHESIS AND PROPERTIES OF [R-(Z)]-(+)-ALPHA-(1-AZABICYCLO[2.2.2]OCT-3-YL)-ALPHA-(METHOXYIMINO) ACETONITRILE, A NOVEL FUNCTIONALLY SELECTIVE MUSCARINIC PARTIAL AGONIST

被引:9
作者
BROMIDGE, SM [1 ]
CASSIDY, F [1 ]
CLARK, MSG [1 ]
EGGLESTON, DS [1 ]
ORIEK, BS [1 ]
机构
[1] SMITHKLINE BEECHAM PHARMACEUT, DISCOVERY RES, DEPT MOLEC NEUROPATHOL, HARLOW CM19 5AD, ESSEX, ENGLAND
关键词
D O I
10.1039/c39940002189
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The (Z)-N-methoxy imidoyl nitrile functionality is a novel methyl ester bioisostere, which, when substituted onto the quinuclidine ring system gives the title compound 1, a stable, brain penetrant and functionally selective muscarinic; partial agonist; X-ray studies confirm the configurational assignment and reveal that the imino and cyano bond lengths are consistent with those expected for formal double and triple bonds, respectively.
引用
收藏
页码:2189 / 2190
页数:2
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