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

PX Franklin1; S Yer; e1; HM Thakar1; GS Inamdar1; RS Giri1; H Padh2; V Sudarsanam2; Kamala K Vasu1

doi:10.4103/0250-474X.56021

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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 perd@perdcentre.com

DOI: 10.4103/0250-474X.56021

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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