STUDIES ON CARDIOTONIC AGENTS .6. SYNTHESIS OF NOVEL 4,5-DIHYDRO-3(2H)-PYRIDAZINONE DERIVATIVES CARRYING SOME BENZOHETEROCYCLES AT THE 6-POSITION

被引:0
|
作者
NOMOTO, Y
TAKAI, H
OHNO, T
KUBO, K
机构
关键词
CARDIOTONIC AGENT; STRUCTURE ACTIVITY RELATIONSHIP; PYRIDAZINONE; QUINAZOLINE; BENZOTHIAZOLE; IMIDAZOBENZOTHIAZOLE; BENZOTHIOPHENE; BENZOTHIENOPYRIMIDINE;
D O I
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中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several benzothiazolyl, imidazobenzothiazolyl, benzothienyl, benzothienopyrimidinyl and quinazolinyl 4,5-dihydro-3(2H)-pyridazinones were synthesized and examined for cardiotonic activity in anesthetized dogs after i.v. administration. Among them, 4-methylamino-7-(2,3,4,5-tetrahydro-5-methyl-3-oxo-6-pyridazinyl)quinazoline (36) showed potent and long-lasting inotropic activity (relative potency = 2.11, milrinone = 1). The activity of 36 was more potent that indolidan (2) (relative potency = 1.53) which is one of the most potent inotropic agents to date.
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页码:352 / 357
页数:6
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