1. Synthesis, anti-inflammatory, ulcerogenic and cyclooxygenase activities of indenopyrimidine derivatives
- Author
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Dattatraya K. Jamale, Sunil S. Vibhute, Laxman S. Walekar, Navanath J. Valekar, Ajinkya A. Patravale, Govind B. Kolekar, Prashant V. Anbhule, Santosh S. Undare, and Madhukar B. Deshmukh
- Subjects
0301 basic medicine ,medicine.drug_class ,Clinical Biochemistry ,Anti-Inflammatory Agents ,Pharmaceutical Science ,Pharmacology ,Carrageenan ,Ulcer index ,01 natural sciences ,Biochemistry ,Anti-inflammatory ,Structure-Activity Relationship ,03 medical and health sciences ,chemistry.chemical_compound ,Catalytic Domain ,Edema ,Drug Discovery ,medicine ,Animals ,Structure–activity relationship ,Cyclooxygenase Inhibitors ,Stomach Ulcer ,Molecular Biology ,Binding Sites ,biology ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,Diclofenac Sodium ,Anti-Ulcer Agents ,Rats ,0104 chemical sciences ,Molecular Docking Simulation ,Pyrimidines ,030104 developmental biology ,Cyclooxygenase 2 ,Docking (molecular) ,Cyclooxygenase 1 ,biology.protein ,Pyrazoles ,Molecular Medicine ,Cyclooxygenase ,medicine.symptom ,Half-Life - Abstract
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.
- Published
- 2016