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Abstract

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

Author(s): PX Franklin1, S Yerande1, HM Thakar1, GS Inamdar1, RS Giri1, H Padh2, V Sudarsanam2, Kamala K Vasu1
1 Medicinal Chemistry Department, B. V. Patel Pharmaceutical Education and Research Development Centre, Thaltej, Ahmedabad-380 054, India 2 Biotechnology Department, B. V. Patel Pharmaceutical Education and Research Development Centre, Thaltej, Ahmedabad-380 054, India

Correspondence Address:
Kamala K Vasu Medicinal Chemistry Department, B. V. Patel Pharmaceutical Education and Research Development Centre, Thaltej, Ahmedabad-380 054 India [email protected]


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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