Synthesis, Antiinflammatory and HIV-1 Integrase Inhibitory Activities of 1,2-Bis[5-thiazolyl]ethane-1,2-dione Derivatives

P X Franklin; S Yerande; H M Thakar; G S Inamdar; R S Giri; H Padh; V Sudarsanam; Kamala K Vasu

doi:10.4103/0250-474X.56021

Synthesis, Antiinflammatory and HIV-1 Integrase Inhibitory Activities of 1,2-Bis[5-thiazolyl]ethane-1,2-dione Derivatives

Indian J Pharm Sci. 2009 May;71(3):259-63. doi: 10.4103/0250-474X.56021.

Authors

P X Franklin¹, S Yerande, H M Thakar, G S Inamdar, R S Giri, H Padh, V Sudarsanam, Kamala K Vasu

Affiliation

¹ Medicinal Chemistry Department, B. V. Patel Pharmaceutical Education and Research Development Centre, Thaltej, Ahmedabad-380 054, India.

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.

Keywords: 1,4-dibromo butane-2,3-dione; N,N-diethyl benzamidine; N,N-diethyl phenylacetamidine; benzoylisothiocyanate.