Synthesis and biological activity of analogs of CPZEN-45, a novel antituberculosis drug.
J Antibiot (Tokyo)
; 72(12): 970-980, 2019 12.
Article
em En
| MEDLINE
| ID: mdl-31471594
ABSTRACT
Analogs of CPZEN-45, which is expected to be a promising new antituberculosis drug that overcomes the shortcomings of caprazamycins, were synthesized and their biological activities were evaluated. The biological activity of analogs 1-3, which converted the anilide portion, and analogs 4 and 5, focusing on the seven-membered ring, were lower than that of CPZEN-45. These results suggest that the inhibitory activity of CPZEN-45 against TagO, an ortholog of WecA, has a strict structural limitation, and it was hoped for elucidation of the mode of action of CPZEN-45 using structural biology in the future.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Relação Estrutura-Atividade
/
Azepinas
/
Mycobacterium
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Antituberculosos
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article