Design, synthesis and characterization of dual inhibitors against new targets FabG4 and HtdX of Mycobacterium tuberculosis.
Eur J Med Chem
; 100: 223-34, 2015 Jul 15.
Article
em En
| MEDLINE
| ID: mdl-26092447
ABSTRACT
Herein, we present dual inhibitors of new targets FabG4 and HtdX for the first time. In this work, eight compounds have been designed, synthesized, characterized and evaluated for bio-activities. Amongst them, six compounds have shown inhibitory activities. Three of them (12-14) demonstrate dual inhibition of both FabG4 and HtdX at low micromolar concentration. In addition, the dual inhibitors show good anti-mycobacterial properties against both planktonic growth and biofilm culture of Mycobacterium species. This study is an important addition to tuberculosis drug discovery because it explores two new enzymes as drug targets and presents their dual inhibitors as good candidates for pre-clinical trials.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
/
Oxirredutases do Álcool
/
Inibidores Enzimáticos
/
Hidroliases
/
Mycobacterium tuberculosis
/
Antituberculosos
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article