title: Synthesis, Antiinflammatory and HIV-1 Integrase Inhibitory Activities of 1,2-Bis[5-thiazolyl]ethane-1,2-dione Derivatives.
abstract: Based on principles of pharmacophore delineation and drug designing, compounds containing diketofunctionallity namely 1,2-bis[5-thiazolyl]ethane-1,2-diones were designed and synthesized as antiinflammatory agents. The compounds were evaluated in carrageenan-induced rat-paw edema method. G-3, G-6, G-17, G-20, G-23, G-22, L-708 and 906 showed good antiinflammatory activity. In addition as diketo functionality containing compounds are reported to have HIV-1 integrase inhibitory property, and these compounds contains diketo functionality, so these compounds were screened in assay for HIV-1 integrase inhibition. Few compounds showed weak HIV-1 integrase Inhibitory activity.
authors.affiliation: Medicinal Chemistry Department, B. V. Patel Pharmaceutical Education and Research Development Centre, Thaltej, Ahmedabad-380 054, India.
authors.forename: P X
authors.initials: PX
authors.lastname: Franklin
authors.forename: S
authors.initials: S
authors.lastname: Yerande
authors.forename: H M
authors.initials: HM
authors.lastname: Thakar
authors.forename: G S
authors.initials: GS
authors.lastname: Inamdar
authors.forename: R S
authors.initials: RS
authors.lastname: Giri
authors.forename: H
authors.initials: H
authors.lastname: Padh
authors.forename: V
authors.initials: V
authors.lastname: Sudarsanam
authors.forename: Kamala K
authors.initials: KK
authors.lastname: Vasu