Chemical and Pharmaceutical Bulletin p. 1692 - 1695 (1995)
Update date:2022-08-03
Topics: Synthetase inhibitors Indole derivatives Thromboxane A2 Histamine H1-blocking activity
Kamiya
Matsui
Shirahase
Nakamura
Wada
Kanda
Shimaji
Kakeya
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).
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