Syntheses and complement inhibitory activities of 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids

The syntheses of 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids are described. These compounds express potent in vitro inhibition of the human classical complement pathway, and qualitative SAR have been determined. Several of the in vitro active compounds also suppressed the complement dep...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1985-02, Vol.28 (2), p.160-164
Main Authors: Bailey, Denis M, DeGrazia, George D, Alexander, E. John, Powles, Ronald G, Johnson, Robert E, Patrick, Richard A, Heerdt, Barbara G, Fairbain, Margo E, Pruden, Donald J
Format: Article
Language:English
Subjects:
Animals
Arthus Reaction
Chemistry
Complement Inactivator Proteins - chemical synthesis
Complement Pathway, Classical - drug effects
Cyclohexanecarboxylic Acids - chemical synthesis
Cyclohexanecarboxylic Acids - pharmacology
Exact sciences and technology
Guinea Pigs
Hemolysis
Heterocyclic compounds
Heterocyclic compounds with only one n hetero atom and condensed derivatives
Humans
Male
Organic chemistry
Preparations and properties
Stereoisomerism
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Summary:The syntheses of 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids are described. These compounds express potent in vitro inhibition of the human classical complement pathway, and qualitative SAR have been determined. Several of the in vitro active compounds also suppressed the complement dependent reverse passive Arthus reaction (RPAR) in guinea pigs.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00380a002