Peptide deformylase inhibitors of Mycobacterium tuberculosis: synthesis, structural investigations, and biological results.
Bioorg Med Chem Lett
; 18(24): 6568-72, 2008 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-19008098
ABSTRACT
Bacterial peptide deformylase (PDF) belongs to a subfamily of metalloproteases catalyzing the removal of the N-terminal formyl group from newly synthesized proteins. We report the synthesis and biological activity of highly potent inhibitors of Mycobacterium tuberculosis (Mtb) PDF enzyme as well as the first X-ray crystal structure of Mtb PDF. Structure-activity relationship and crystallographic data clarified the structural requirements for high enzyme potency and cell based potency. Activities against single and multi-drug-resistant Mtb strains are also reported.
Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Tuberculose
/
Amidoidrolases
/
Mycobacterium tuberculosis
/
Antituberculosos
Limite:
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article