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J Med Chem ; 63(3): 1105-1131, 2020 02 13.
Artigo em Inglês | MEDLINE | ID: mdl-31904960

RESUMO

A series of derivatives of the antimycobacterial natural product pyridomycin have been prepared with the C2 side chain attached to the macrocyclic core structure by a C-C single bond, in place of the synthetically more demanding enol ester double bond found in the natural product. Hydrophobic C2 substituents of sufficient size generally provide for potent anti-Mtb activity of these dihydropyridomycins (minimum inhibitory concentration (MIC) values around 2.5 µM), with several analogs thus approaching the activity of natural pyridomycin. Surprisingly, some of these compounds, in contrast to pyridomycin, are insensitive to overexpression of InhA in Mycobacterium tuberculosis (Mtb). This indicates that their anti-Mtb activity does not critically depend on the inhibition of InhA and that their overall mode of action may differ from that of the original natural product lead.


Assuntos
Antituberculosos/farmacologia , Inibidores Enzimáticos/farmacologia , Oligopeptídeos/farmacologia , Antituberculosos/síntese química , Antituberculosos/química , Proteínas de Bactérias/antagonistas & inibidores , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Mycobacterium tuberculosis/efeitos dos fármacos , Oligopeptídeos/síntese química , Oligopeptídeos/química , Oxirredutases/antagonistas & inibidores , Relação Estrutura-Atividade
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