Synthesis and Antitubercular Evaluation of New Bis-1,2,3-Triazoles Derived from D-Mannitol |
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| Authors: | Marcelle de L Ferreira Marcus V N de Souza Solange M S V Wardell James L Wardell Thatyana R A Vasconcelos Vitor F Ferreira |
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| Institution: | 1. Funda??o Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos , Funda??o Oswaldo Cruz , 21041-250, Rio de Janeiro, RJ, Brazil;2. Universidade Federal Fluminense, Instituto de Química, Departamento de Química Organica, Outeiro de S. Jo?o Batista s/n° Centro , 24020-150, Niterói, RJ, Brazil;3. Funda??o Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos , Funda??o Oswaldo Cruz , 21041-250, Rio de Janeiro, RJ, Brazil;4. Universidade Federal Fluminense, Instituto de Química, Departamento de Química Organica, Outeiro de S. Jo?o Batista s/n° Centro , 24020-150, Niterói, RJ, Brazil |
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| Abstract: | Five new bis-1,2,3-triazole derivatives from D-mannitol, namely 2,3,4,5-tetra-O-acetyl-1,6-dideoxy-1,6-bis-(4-substituted-1H-1,2,3-triazol-1-yl)-D-mannitol (4), have been synthesized from 2,3,4,5-tetra-O-acetyl-1,6-diazido-1,6-dideoxy-D-mannitol (3) and alkynes, employing copper (I)-catalyzed azide-alkyne cycloaddition (CuAAC) methodology. Evaluation of their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv using the Alamar Blue susceptibility test indicated poor activities. However, this study has provided information about the SAR of D-mannitol derivatives in the search for new anti-TB drugs based on this carbohydrate. |
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| Keywords: | D-mannitol 1 2 3-Triazole Antitubercular activity Drugs |
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