具有组胺H1阻断活性的血栓素A2合成酶抑制剂：一系列新型吲哚衍生物的合成与评价
Thromboxane A2 synthetase inhibitors with histamine H1-blocking activity: synthesis and evaluation of a new series of indole derivatives.
作者信息
Kamiya S, Matsui H, Shirahase H, Nakamura S, Wada K, Kanda M, Shimaji H, Kakeya N
机构信息
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd., Japan.
出版信息
Chem Pharm Bull (Tokyo). 1995 Oct;43(10):1692-5. doi: 10.1248/cpb.43.1692.
A novel series of N-substituted 3-(1H-imidazol-1-ylmethyl)indole carboxylic acid derivatives were prepared and evaluated for thromboxane A2 (TXA2) synthetase-inhibitory and histaminergic H1-blocking activity. Among the compounds synthesized, indole-6-carboxylic acid derivatives showed higher activities than the other positional isomers of carboxylic acid. 1-[3-(4-Benzhydryl-1-piperazinyl)propyl]-3-(1H-imidazol-1-ylmethyl )-1H-indole-6-carboxylic acid (12) had the strongest thromboxane synthetase inhibitory activity (IC50 = 5 x 10(-8) M) and H1-blocking activity (IC50 = 8 x 10(-9) M).
制备了一系列新型的N-取代的3-(1H-咪唑-1-基甲基)吲哚羧酸衍生物，并对其血栓素A2（TXA2）合成酶抑制活性和组胺能H1阻断活性进行了评估。在合成的化合物中，吲哚-6-羧酸衍生物显示出比羧酸的其他位置异构体更高的活性。1-[3-(4-二苯甲基-1-哌嗪基)丙基]-3-(1H-咪唑-1-基甲基)-1H-吲哚-6-羧酸（12）具有最强的血栓素合成酶抑制活性（IC50 = 5×10(-8) M）和H1阻断活性（IC50 = 8×10(-9) M）。
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