CARDIOTONIC-C RING MODIFIED ISOMAZOLE ANALOGS

被引:5
作者
BARRACLOUGH, P
BLACK, JW
CAMBRIDGE, D
DEMAINE, DA
GERSKOWITCH, VP
GILES, H
HILL, AP
HULL, RAD
LYER, R
KING, WR
LIVINGSTONE, DJ
NOBBS, MS
RANDALL, P
SHAH, GP
WHITING, MV
机构
[1] WELLCOME RES LABS,DEPT PHARMACOL,BECKENHAM BR3 3BS,KENT,ENGLAND
[2] WELLCOME RES LABS,DEPT PHYS SCI,BECKENHAM BR3 3BS,KENT,ENGLAND
关键词
D O I
10.1002/ardp.19903230812
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Isomazole analogues which have achiral electron withdrawing substituents at the 4′‐position and analogues with heterocyclic ‘C’ rings have been synthesized and evaluated as inotropic agents. It was found that pyridyl could replace phenyl in the ‘C’ ring without loss of activity. The 4′‐methylsulphonyl, ‐cyano, ‐carboxamido, and acetyl analogues had similar inotropic potencies to Isomazole whilst displaying superior cardiovascular profiles in in vivo studies. Copyright © 1990 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim
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页码:507 / 512
页数:6
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