Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
8993397 | Il Farmaco | 2005 | 10 Pages |
Abstract
The present study focuses on development of new potential inhibitors of cyclooxygenase-2 (COX-2): series of N-pyrrolylcarboxylic acids. 3D-QSAR (Quantitative Structure-Activity Relationship) CoMFA (Comparative Molecular Field Analysis) and CoMSIA (Comparative Molecular Similarity Index Analysis) models for predicting inhibitory activities against COX-1 and COX-2 as well as for evaluating in vivo anti-inflammatory activity were obtained and used for preliminary screening of new anti-inflammatory N-pyrrolylcarboxylic acids. Nine compounds were selected for in vivo testing and evaluated for their potency to decrease carrageenin-induced edema in rats. The compounds were applied i.p. at doses 20Â mg/kg and 40Â mg/kg and p.o. at doses 10Â mg/kg and 40Â mg/kg. Six compounds showed more than 70% protection of the edema. Indomethacin (2Â mg/kg i.p.), used as a reference drug, possessed 54% anti-inflammatory activity under similar experimental conditions.
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Authors
Iglika Lessigiarska, Atanas Nankov, Adriana Bocheva, Ilza Pajeva, Atanas Bijev,