1,3-Azoles from Ortho-naphthoquinones: Synthesis of Aryl Substituted Imidazoles and Oxazoles and Their Potent Activity Against Mycobacterium Tuberculosis

Overview

Journal Bioorg Med Chem

Specialties Biochemistry
Chemistry

Date 2012 Sep 25

PMID 23000294

Citations 6

Authors

Kelly C G Moura

Paula F Carneiro

Maria do Carmo F R Pinto

Jose A da Silva

Valeria R S Malta

Carlos A De Simone

Gleiston G Dias

Guilherme A M Jardim

Jessica Cantos

Tatiane S Coelho

Pedro E Almeida Da Silva

Eufranio N da Silva Jr

Affiliations

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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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