Yamaguchi M, Maruyama N, Koga T, Kamei K, Akima M, Kuroki T, Hamana M, Ohi N
Fuji-gotemba Research Laboratories, Chugai Pharmaceutical Company, Ltd., Shizuoka, Japan.
Chem Pharm Bull (Tokyo). 1995 Feb;43(2):236-40. doi: 10.1248/cpb.43.236.
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.
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。