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Synthesis and in vitro anti-HIV activity of N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives using MTT method

2011; Elsevier BV; Volume: 21; Issue: 11 Linguagem: Inglês

10.1016/j.bmcl.2011.03.105

1464-3405

Dhairya Bhavsar, Jalpa C. Trivedi, Shrey Parekh, Mahesh M. Savant, Shailesh Thakrar, Abhay Bavishi, Ashish Radadiya, Hardevsinh Vala, Jignesh Lunagariya, Manisha Parmar, Ladwa Paresh, Roberta Loddo, Anamik Shah,

Synthesis and biological activity

A series of novel N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives has been synthesized. All the newly synthesized compounds were evaluated for their anti-HIV activity using MTT method. Most of these compounds showed moderate to potent activity against wild-type HIV-1 with an EC50 ranging from >7 EC50 [μg/ml] to <100 EC50 [μg/ml]. Among them, N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide 6v was identified as the most promising compound (EC50 = <7 μg/ml). Among all the compounds, three compounds 6m, 6v and 6u have been exhibits potent anti-HIV activity against MT-4 cells.