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1,3-Azoles from ortho-naphthoquinones: Synthesis of aryl substituted imidazoles and oxazoles and their potent activity against Mycobacterium tuberculosis |
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| Authors: | Kelly CG Moura Paula F Carneiro Maria do Carmo FR Pinto José A da Silva Valéria RS Malta Carlos A de Simone Gleiston G Dias Guilherme AM Jardim Jéssica Cantos Tatiane S Coelho Pedro E Almeida da Silva Eufrânio N da Silva |
| Institution: | 1. Núcleo de Pesquisas de Produtos Naturais, UFRJ, 21944-971 Rio de Janeiro, RJ, Brazil;2. Instituto de Química e Biotecnologia, UFAL, 57072-970 Maceió, AL, Brazil;3. Departamento de Física e Informática, Instituto de Física, USP, 13560-970 São Carlos, SP, Brazil;4. Laboratório de Química Sintética e Heterocíclica, Instituto de Ciências Exatas, Departamento de Química, UFMG, 31270-901 Belo Horizonte, MG, Brazil;5. Laboratório de Micobacterias, Faculdade de Medicina, FURG, 96200-190 Rio Grande, RS, Brazil |
| Abstract: | Twenty-three naphthoimidazoles and six naphthoxazoles were synthesised and evaluated against susceptible and rifampicin- and isoniazid-resistant strains of Mycobacterium tuberculosis. Among all the compounds evaluated, fourteen presented MIC values in the range of 0.78 to 6.25 μg/mL against susceptible and resistant strains of M. tuberculosis. Five structures were solved by X-ray crystallographic analysis. These substances are promising antimycobacterial prototypes. |
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