Undare Santosh S, Valekar Navanath J, Patravale Ajinkya A, Jamale Dattatraya K, Vibhute Sunil S, Walekar Laxman S, Kolekar Govind B, Deshmukh M B, Anbhule Prashant V
Medicinal Chemistry Research Lab., Department of Chemistry, Shivaji University, Kolhapur 416004, M.S., India.
Shri Shivaji Mahavidyalaya, Barshi, M.S., India.
Bioorg Med Chem Lett. 2016 Feb 1;26(3):814-818. doi: 10.1016/j.bmcl.2015.12.088. Epub 2015 Dec 28.
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.
本研究的目的是评估茚并嘧啶衍生物的抗炎、致溃疡作用及环氧化酶活性。通过角叉菜胶诱导的大鼠足趾肿胀试验研究受试化合物的抗炎活性。化合物A1、A6、A7和A12表现出与标准药物双氯芬酸钠（85.33%）相当的抗炎活性（79.33 - 81.33%），而A6、A7、A9、A12和A14的溃疡指数比参考标准双氯芬酸钠更好。为了阐明抗炎活性，进行对接实验以研究这些化合物与COX - 2酶活性位点结合的能力。
