Synthesis and preliminary biological evaluation of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives as potential antimycobacterial agents: an operational Topliss Tree approach |
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Authors: | Kakwani Manoj D Palsule Desai Nutan H Lele Arundhati C Ray Muktikant Rajan M G R Degani Mariam S |
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Affiliation: | Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai 400 019, India. |
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Abstract: | A series of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives were designed on basis of structural similarity to the known FAS II inhibitors. Topliss operational method was used to optimize the potency of molecules. The minimum inhibitory concentration (MIC) of all synthesized compounds was determined against Mycobacterium tuberculosis H(37)R(v) using resazurin microtitre assay (REMA) plate method. The synthesized compounds exhibit antimycobacterial activity in the range of 5-95μM with a good safety profile. |
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Keywords: | Mycobacterium tuberculosis FAS II Triazoles Topliss tree |
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