Synthesis, anti-inflammatory, ulcerogenic and cyclooxygenase activities of indenopyrimidine derivatives

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• 作者：Santosh S. Undare^a ; Navanath J. Valekar^a ; Ajinkya A. Patravale^a ; Dattatraya K. Jamale^b ; Sunil S. Vibhute^b ; Laxman S. Walekar^a ; Govind B. Kolekar^a ; M.B. Deshmukh^a ; Prashant V. Anbhule^a ; ^{pvanbhule@gmail.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Indenopyrimidine ; Anti-inflammatory ; Anti-ulcerogenic ; COX-2 ; Molecular docking
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 February 2016
• 年：2016
• 卷：26
• 期：3
• 页码：814-818
• 全文大小：790 K

文摘

Objective of the present work was to evaluate the anti-inflammatory, ulcerogenicity and cyclooxygenase activity of indenopyrimidine derivatives. Anti-inflammatory activity of the tested compounds is investigated by carrageenan-induced rat paw edema assay. Compounds A1, A6, A7 and A12 exhibit the comparable anti-inflammatory activity (79.33–81.33%) to the standard drug diclofenac sodium (85.33%), while A6, A7, A9, A12 and A14 show better ulcer index than the reference standard diclofenac sodium. To rationalize the anti-inflammatory activity, docking experiments are performed to study the ability of these compounds to bind into the active site of COX-2 enzyme.