title: Synthesis, anti-inflammatory, ulcerogenic and cyclooxygenase activities of indenopyrimidine derivatives.
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.
authors.affiliation: Medicinal Chemistry Research Lab., Department of Chemistry, Shivaji University, Kolhapur 416004, M.S., India.
authors.forename: Santosh S
authors.initials: SS
authors.lastname: Undare
authors.affiliation: Medicinal Chemistry Research Lab., Department of Chemistry, Shivaji University, Kolhapur 416004, M.S., India.
authors.forename: Navanath J
authors.initials: NJ
authors.lastname: Valekar
authors.affiliation: Medicinal Chemistry Research Lab., Department of Chemistry, Shivaji University, Kolhapur 416004, M.S., India.
authors.forename: Ajinkya A
authors.initials: AA
authors.lastname: Patravale
authors.affiliation: Shri Shivaji Mahavidyalaya, Barshi, M.S., India.
authors.forename: Dattatraya K
authors.initials: DK
authors.lastname: Jamale
authors.affiliation: Shri Shivaji Mahavidyalaya, Barshi, M.S., India.
authors.forename: Sunil S
authors.initials: SS
authors.lastname: Vibhute
authors.affiliation: Medicinal Chemistry Research Lab., Department of Chemistry, Shivaji University, Kolhapur 416004, M.S., India.
authors.forename: Laxman S
authors.initials: LS
authors.lastname: Walekar
authors.affiliation: Medicinal Chemistry Research Lab., Department of Chemistry, Shivaji University, Kolhapur 416004, M.S., India.
authors.forename: Govind B
authors.initials: GB
authors.lastname: Kolekar
authors.affiliation: Medicinal Chemistry Research Lab., Department of Chemistry, Shivaji University, Kolhapur 416004, M.S., India.
authors.forename: M B
authors.initials: MB
authors.lastname: Deshmukh
authors.affiliation: Medicinal Chemistry Research Lab., Department of Chemistry, Shivaji University, Kolhapur 416004, M.S., India. Electronic address: pvanbhule@gmail.com.
authors.forename: Prashant V
authors.initials: PV
authors.lastname: Anbhule
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D001665:Binding Sites; D002351:Carrageenan / Q000633:toxicity; D020134:Catalytic Domain; D051545:Cyclooxygenase 1 / Q000737:chemistry* / Q000378:metabolism; D051546:Cyclooxygenase 2 / Q000737:chemistry* / Q000378:metabolism; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D006207:Half-Life; D062105:Molecular Docking Simulation; D011720:Pyrazoles / Q000737:chemistry; D011743:Pyrimidines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D051381:Rats; D013276:Stomach Ulcer / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000893:Anti-Inflammatory Agents; D000897:Anti-Ulcer Agents; D016861:Cyclooxygenase Inhibitors; D011720:Pyrazoles; D011743:Pyrimidines; D002351:Carrageenan; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C030986:pyrimidine
keywords: Anti-inflammatory; Anti-ulcerogenic; COX-2; Indenopyrimidine; Molecular docking