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

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-...

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Bibliographic Details
Published in:Indian journal of pharmaceutical sciences 2009-05, Vol.71 (3), p.259-263
Main Authors: Franklin, P X, Yerande, S, Thakar, H M, Inamdar, G S, Giri, R S, Padh, H, Sudarsanam, V, Vasu, Kamala K
Format: Article
Language:English
Subjects:
Binding sites
Deoxyribonucleic acid
Disease
DNA
Drug therapy
Research Paper
Rheumatoid arthritis
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Summary: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.
ISSN:0250-474X
1998-3743
DOI:10.4103/0250-474X.56021