کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8993397 | 1113797 | 2005 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
3D-QSAR and preliminary evaluation of anti-inflammatory activity of series of N-pyrrolylcarboxylic acids
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موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Il Farmaco - Volume 60, Issue 3, March 2005, Pages 209-218
Journal: Il Farmaco - Volume 60, Issue 3, March 2005, Pages 209-218
نویسندگان
Iglika Lessigiarska, Atanas Nankov, Adriana Bocheva, Ilza Pajeva, Atanas Bijev,