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具有血栓素A2合成酶抑制和支气管扩张双重活性的新型抗哮喘药。IV. 2-[2-(1-咪唑基)乙基]-4-(3-吡啶基)-1(2H)-酞嗪酮

Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. IV. 2-[2-(1-Imidazolyl)ethyl]-4-(3-pyridyl)-1(2H)-phthalazinones.

作者信息

Yamaguchi M, Koga T, Kamei K, Akima M, Maruyama N, Kuroki T, Hamana M, Ohi N

机构信息

Fuji-gotemba Research Laboratories, Chugai Pharmaceutical Company, Ltd., Shizuoka, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1994 Sep;42(9):1850-3. doi: 10.1248/cpb.42.1850.

DOI:10.1248/cpb.42.1850
PMID:7954937
Abstract

Synthesis and pharmacological evaluation of several compounds related to 2-[2-(1-imidazolyl)ethyl]-4-(3-pyridyl)-1(2H)-phthalazinones are described. The phenyl moiety of the phthalazinone skeleton was found to play an important role in both thromboxane A2 synthetase-inhibitory and bronchodilatory activities. Further, the 3-pyridyl group at the 4-position was shown to be necessary for in vivo thromboxane A2 synthetase-inhibitory activity.

摘要

描述了几种与2-[2-(1-咪唑基)乙基]-4-(3-吡啶基)-1(2H)-酞嗪酮相关化合物的合成及药理评价。发现酞嗪酮骨架的苯基部分在血栓素A2合成酶抑制活性和支气管扩张活性中均起重要作用。此外，4位的3-吡啶基对于体内血栓素A2合成酶抑制活性是必需的。

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