Syntheses and complement inhibitory activities of 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids
- 1 February 1985
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 28 (2) , 160-164
- https://doi.org/10.1021/jm00380a002
Abstract
The syntheses of 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids [4-(2-phenyl-1H-indol-3-yl)-3-cyclohexene-1-carboxylic acid, 4-(2-phenyl-1H-indol-3-yl)-3-cyclohexene-1,1-dicarboxylic acid, 4-(1-methyl-2-phenyl-1H-indol-3-yl)-3-cyclohexene-1,1-dicarboxylic acid, 4-(1-methyl-2-phenyl-1H-indol-3-yl)-3-cyclohexane-1-carboxylic acid, 4-(1-ethyl-2-phenyl-1H-indol-3-yl)-3-cyclohexene-1-carboxylic acid, 4-(2-phenyl-1-propyl-1H-indol-3-yl)-3-cyclohexene-1-carboxylic acid, 4-(1-ethyl-2-phenyl-1H-indol-3-yl)-3-cyclohexene-1,1-dicarboxylic acid, 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1,1-dicarboxylic acid, 4-(1-methyl-2-phenyl-1H-indol-3-yl)cyclohexane-1,1-dicarboxylic acid, cis-trans-4-(1-methyl-2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acid, cis-4-(1-methyl-2-phenyl-1H-indol-3-yl)-1,1-cyclohexane dicarboxylic acid, 4-(2-phenyl-1H-indol-3-yl)benzoic acid and 4-(1-methyl-2-phenyl-1H-indol-3-yl)benzoic acid] are described. These compounds expressed potent in vitro inhibition of the human classical complement pathway, and qualitative SAR [structure-activity relationship] was determined. Several of the in vitro compounds also suppressed the complement dependent reverse passive Arthus reactin (RPAR) in guinea pigs.This publication has 1 reference indexed in Scilit:
- Inhibition of the Alternative Pathway of Complement by Gold Sodium Thiomalate in VitroThe Journal of Immunology, 1978