In Vitro Efficacies, ADME, and Pharmacokinetic Properties of Phenoxazine Derivatives Active against Mycobacterium tuberculosis.
Antimicrob Agents Chemother
; 63(11)2019 11.
Article
en En
| MEDLINE
| ID: mdl-31427302
ABSTRACT
Mycobacterium tuberculosis, the causative agent of tuberculosis, remains a leading infectious killer globally, demanding the urgent development of faster-acting drugs with novel mechanisms of action. Riminophenazines such as clofazimine are clinically efficacious against both drug-susceptible and drug-resistant strains of M. tuberculosis We determined the in vitro anti-M. tuberculosis activities, absorption, distribution, metabolism, and excretion properties, and in vivo mouse pharmacokinetics of a series of structurally related phenoxazines. One of these, PhX1, displayed promising drug-like properties and potent in vitro efficacy, supporting its further investigation in an M. tuberculosis-infected animal model.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Oxazinas
/
Mycobacterium tuberculosis
/
Antituberculosos
Límite:
Animals
Idioma:
En
Año:
2019
Tipo del documento:
Article