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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。V. 噻吩并哒嗪酮衍生物。

Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. V. Thienopyridazinone derivatives.

作者信息

Yamaguchi M, Maruyama N, Koga T, Kamei K, Akima M, 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). 1995 Feb;43(2):236-40. doi: 10.1248/cpb.43.236.

DOI:10.1248/cpb.43.236
PMID:7728930
Abstract

Synthesis and pharmacological evaluation of novel thienopyridazinones and related compounds are described. A thiophene ring was found to be able to replace the benzene ring of a phthalazinone without loss of biological activities. This observation supports our hypothesis that the benzene ring plays an important role in both thromboxane A2 (TXA2) synthetase-inhibitory and bronchodilatory activities. Further, it was shown that the carbonyl moiety of a phthalazinone is not necessary for these activities.

摘要

本文描述了新型噻吩并哒嗪酮及相关化合物的合成与药理评价。研究发现，噻吩环能够取代酞嗪酮的苯环，且不会丧失生物活性。这一观察结果支持了我们的假设，即苯环在血栓素A2（TXA2）合成酶抑制活性和支气管扩张活性中均起重要作用。此外，研究表明，酞嗪酮的羰基部分对于这些活性并非必需。

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