Bioorganic & Medicinal Chemistry 2012-11-01

1,3-Azoles from ortho-naphthoquinones: synthesis of aryl substituted imidazoles and oxazoles and their potent activity against Mycobacterium tuberculosis.

Kelly C G Moura, Paula F Carneiro, Maria do Carmo F R Pinto, José A da Silva, Valéria R S Malta, Carlos A de Simone, Gleiston G Dias, Guilherme A M Jardim, Jéssica Cantos, Tatiane S Coelho, Pedro E Almeida da Silva, Eufrânio N da Silva

文献索引：Bioorg. Med. Chem. 20(21) , 6482-8, (2012)

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摘要

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.Copyright © 2012 Elsevier Ltd. All rights reserved.