期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 81, 期 5, 页码 591-599出版社
WILEY
DOI: 10.1111/cbdd.12101
关键词
[1,2,4]triazolo[3,4-a]phthalazine; positive inotropic activity; stroke volume; tetrazolo[5,1-a]phthalazine
资金
- National Science Foundation of China [81160381]
Two series of [1,2,4]triazolo[3,4-a]phthalazine and tetrazolo[5,1-a]phthalazine derivatives bearing substituted benzylpiperazine moieties have been synthesized and evaluated for their positive inotropic activity by measuring left atrium stroke volume on isolated rabbit heart preparations. The majority of the derivatives exhibited better in vitro activity than the existing drug, milrinone, and 6-((4-(4-methoxyphenyl)piperazin-1-yl)methyl)tetrazolo[5,1-a]phthalazine. 8m in particular was identified as the most potent with an increased stroke volume of 12.02 +/- 0.20% (milrinone: 2.46 +/- 0.07%) at a concentration of 3x105m. The chronotropic effects of the compounds that exhibited good potency were also evaluated.
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