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Studies on cardiotonic agents. VI. Synthesis of novel 4,5-dihydro-3(2H)-pyridazinone derivatives carrying some benzoheterocycles at the 6-position.

作者信息

Nomoto Y, Takai H, Ohno T, Kubo K

机构信息

Pharmaceutical Research Laboratories, Fuji Kyowa Hakko Kogyo Co., Ltd., Shizuoka, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1991 Feb;39(2):352-7. doi: 10.1248/cpb.39.352.

DOI:10.1248/cpb.39.352
PMID:2054859
Abstract

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 than indolidan (2) (relative potency = 1.53) which is one of the most potent inotropic agents to date.

摘要

相似文献

1
Studies on cardiotonic agents. VI. Synthesis of novel 4,5-dihydro-3(2H)-pyridazinone derivatives carrying some benzoheterocycles at the 6-position.
Chem Pharm Bull (Tokyo). 1991 Feb;39(2):352-7. doi: 10.1248/cpb.39.352.
2
Cardiotonic agents. 2. Synthesis and structure-activity relationships of 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones: a new class of positive inotropic agents.
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Design, synthesis and structure-activity relationship studies of 6-phenyl-4,5-dihydro-3(2H)-pyridazinone derivatives as cardiotonic agents.作为强心剂的6-苯基-4,5-二氢-3(2H)-哒嗪酮衍生物的设计、合成及构效关系研究
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