强心剂。3. 新型6-（取代的1H-咪唑-4（5）-基）-3（2H）-哒嗪酮的合成及生物活性

Cardiotonic agents. 3. Synthesis and biological activity of novel 6-(substituted 1H-imidazol-4(5)-yl)-3(2H)-pyridazinones.

作者信息

Sircar I, Bobowski G, Bristol J A, Weishaar R E, Evans D B

出版信息

J Med Chem. 1986 Feb;29(2):261-7. doi: 10.1021/jm00152a015.

DOI:10.1021/jm00152a015

Abstract

Several 6-(substituted 1H-imidazol-4(5)-yl)-3(2H)-pyridazinones were synthesized and evaluated for positive inotropic activity. The 1H-imidazol-4-yl regioisomers 4,5-dihydro-6-(1-methyl-2-phenyl-1H-imidazol-4-yl)-3(2H)-pyridazinone (25a) and 6-(1-methyl-2-phenyl-1H-imidazol-4-yl)-3(2H)-pyridazinone (28a) were potent positive inotropic agents. By contrast, the corresponding 1H-imidazol-5-yl regioisomers 25b and 28b were only weak positive inotropic agents. Compounds 25a and 28a were also potent inhibitors of cardiac phosphodiesterase fraction III.

摘要

合成了几种6 -（取代的1H -咪唑-4（5）-基）-3（2H）-哒嗪酮，并对其正性肌力活性进行了评估。1H -咪唑-4 -基区域异构体4,5 -二氢-6 -（1 -甲基-2 -苯基-1H -咪唑-4 -基）-3（2H）-哒嗪酮（25a）和6 -（1 -甲基-2 -苯基-1H -咪唑-4 -基）-3（2H）-哒嗪酮（28a）是强效正性肌力药。相比之下，相应的1H -咪唑-5 -基区域异构体25b和28b只是弱正性肌力药。化合物25a和28a也是心脏磷酸二酯酶Ⅲ组分的强效抑制剂。

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