1027073-83-1Relevant articles and documents
Thromboxane A2 synthetase inhibitors with histamine H1-blocking activity: Synthesis and evaluation of a new series of indole derivatives
Kamiya,Matsui,Shirahase,Nakamura,Wada,Kanda,Shimaji,Kakeya
, p. 1692 - 1695 (2007/10/03)
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).