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1,2-双[5-噻唑基]乙烷-1,2-二酮衍生物的合成、抗炎及HIV-1整合酶抑制活性

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

作者信息

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

机构信息

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

出版信息

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

DOI:10.4103/0250-474X.56021
PMID:20490291
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2865783/
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.

摘要

基于药效团描绘和药物设计原理，设计并合成了含有二酮官能团的化合物，即1,2 - 双[5 - 噻唑基]乙烷 - 1,2 - 二酮作为抗炎剂。采用角叉菜胶诱导的大鼠足趾肿胀法对这些化合物进行了评价。G - 3、G - 6、G - 17、G - 20、G - 23、G - 22、L - 708和906表现出良好的抗炎活性。此外，由于据报道含有二酮官能团的化合物具有HIV - 1整合酶抑制特性，而这些化合物含有二酮官能团，因此对这些化合物进行了HIV - 1整合酶抑制测定筛选。少数化合物表现出较弱的HIV - 1整合酶抑制活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f2f3/2865783/564200a9df7e/IJPhS-71-259-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f2f3/2865783/d86f3062c922/IJPhS-71-259-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f2f3/2865783/22f483613c18/IJPhS-71-259-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f2f3/2865783/564200a9df7e/IJPhS-71-259-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f2f3/2865783/d86f3062c922/IJPhS-71-259-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f2f3/2865783/22f483613c18/IJPhS-71-259-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f2f3/2865783/564200a9df7e/IJPhS-71-259-g003.jpg

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