alexa Abstract | Synthesis, antiinflammatory and HIV-1 integrase inhibitory activities of 1,2-bis[5-thiazolyl]ethane-1,2-dione derivatives

Indian Journal of Pharmaceutical Sciences
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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.

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Author(s): PX Franklin S Yerande HM Thakar GS Inamdar RS Giri H Padh V Sudarsanam Kamala K Vasu


N,N-diethyl benzamidine, N,N-diethyl phenylacetamidine, 1,4-dibromo butane-2,3-dione, benzoylisothiocyanate

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