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Arch Pharm (Weinheim) ; 351(12): e1800177, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30407647

RESUMO

New therapeutics are urgently needed to fight tuberculosis and mycobacteria-related diseases that are a major health hazard especially in poor countries. Natural products have been the source of important antitubercular drugs in the past and still need to receive attention as a potent reservoir of chemical structures. Fifteen known and two new (+)-usnic acid (a benzofurandione formerly isolated from lichens) enamines and hydrazones are here described and tested against sensitive and multidrug-resistant strains of mycobacteria. Among several (+)-usnic acid conjugates, PS14 and PS18 showed potent activity against both susceptible and resistant Mycobacterium tuberculosis strains (MIC values of 1-32 and 2-32 mg/L, respectively) comparable with MIC of other antitubercular drugs already in use for tuberculosis treatment.


Assuntos
Antibacterianos/síntese química , Benzofuranos/síntese química , Desenho de Fármacos , Mycobacterium tuberculosis/efeitos dos fármacos , Antibacterianos/química , Antibacterianos/farmacologia , Benzofuranos/química , Benzofuranos/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Farmacorresistência Bacteriana/efeitos dos fármacos , Farmacorresistência Bacteriana/genética , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Mycobacterium/efeitos dos fármacos , Mycobacterium/genética , Mycobacterium tuberculosis/genética
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