Synthesis and in vitro anti Mycobacterium tuberculosis activity of a series of phthalimide derivatives |
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Authors: | Jean L Santos Paulo R Yamasaki Chung Man Chin Célio H Takashi Fernando R Pavan Clarice QF Leite |
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Institution: | 1. Lapdesf—Laboratório de Pesquisa e Desenvolvimento de Fármacos, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista ‘Júlio de Mesquita Filho’, Rod. Araraquara-Jaú Km.01 s/n, Campus, 1480 1-902, Araraquara, SP, Brazil;2. Departamento de Ciências Biológicas, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista ‘Júlio de Mesquita Filho’, Rod. Araraquara-Jaú Km.01 s/n, Campus, 14801-902, Araraquara, SP, Brazil |
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Abstract: | New phthalimide derivatives were easily prepared through condensation of phthalic anhydride and selected amines with variable yields (70–90%). All compounds (3a–l) were evaluated against Mycobacterium tuberculosis H37Rv using Alamar Blue susceptibility. The compounds 3c, 3i, and 3l have the minimum inhibitory concentrations (MICs) of 3.9, 7.8, and 5.0 μg/mL, respectively, and could be considered new lead compounds in the treatment of tuberculosis and multi-drug resistant tuberculosis. |
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