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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Autores principales: Franklin, P. X., Yerande, S., Thakar, H. M., Inamdar, G. S., Giri, R. S., Padh, H., Sudarsanam, V., Vasu, Kamala K.
Formato: Texto
Lenguaje:English
Publicado: Medknow Publications 2009
Materias:
Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2865783/
https://www.ncbi.nlm.nih.gov/pubmed/20490291
http://dx.doi.org/10.4103/0250-474X.56021
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author Franklin, P. X.
Yerande, S.
Thakar, H. M.
Inamdar, G. S.
Giri, R. S.
Padh, H.
Sudarsanam, V.
Vasu, Kamala K.
author_facet Franklin, P. X.
Yerande, S.
Thakar, H. M.
Inamdar, G. S.
Giri, R. S.
Padh, H.
Sudarsanam, V.
Vasu, Kamala K.
author_sort Franklin, P. X.
collection PubMed
description 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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spelling pubmed-28657832010-05-20 Synthesis, Antiinflammatory and HIV-1 Integrase Inhibitory Activities of 1,2-Bis[5-thiazolyl]ethane-1,2-dione Derivatives Franklin, P. X. Yerande, S. Thakar, H. M. Inamdar, G. S. Giri, R. S. Padh, H. Sudarsanam, V. Vasu, Kamala K. Indian J Pharm Sci Research Paper 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. Medknow Publications 2009 /pmc/articles/PMC2865783/ /pubmed/20490291 http://dx.doi.org/10.4103/0250-474X.56021 Text en © Indian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/2.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Paper
Franklin, P. X.
Yerande, S.
Thakar, H. M.
Inamdar, G. S.
Giri, R. S.
Padh, H.
Sudarsanam, V.
Vasu, Kamala K.
Synthesis, Antiinflammatory and HIV-1 Integrase Inhibitory Activities of 1,2-Bis[5-thiazolyl]ethane-1,2-dione Derivatives
title Synthesis, Antiinflammatory and HIV-1 Integrase Inhibitory Activities of 1,2-Bis[5-thiazolyl]ethane-1,2-dione Derivatives
title_full Synthesis, Antiinflammatory and HIV-1 Integrase Inhibitory Activities of 1,2-Bis[5-thiazolyl]ethane-1,2-dione Derivatives
title_fullStr Synthesis, Antiinflammatory and HIV-1 Integrase Inhibitory Activities of 1,2-Bis[5-thiazolyl]ethane-1,2-dione Derivatives
title_full_unstemmed Synthesis, Antiinflammatory and HIV-1 Integrase Inhibitory Activities of 1,2-Bis[5-thiazolyl]ethane-1,2-dione Derivatives
title_short Synthesis, Antiinflammatory and HIV-1 Integrase Inhibitory Activities of 1,2-Bis[5-thiazolyl]ethane-1,2-dione Derivatives
title_sort synthesis, antiinflammatory and hiv-1 integrase inhibitory activities of 1,2-bis[5-thiazolyl]ethane-1,2-dione derivatives
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2865783/
https://www.ncbi.nlm.nih.gov/pubmed/20490291
http://dx.doi.org/10.4103/0250-474X.56021
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