Preparation and antitubercular activities in vitro and in vivo of novel Schiff bases of isoniazid.
Eur J Med Chem
; 44(10): 4169-78, 2009 Oct.
Article
en En
| MEDLINE
| ID: mdl-19524330
ABSTRACT
Structural modification of the frontline antitubercular isonicotinic acid hydrazide (INH) provides lipophilic adaptations (3-46) of the drug in which the hydrazine moiety of the parent compound has been chemically blocked from the deactivating process of N(2)-acetylation by N-arylaminoacetyl transferases. As a class, these compounds show high levels of activity against Mycobacterium tuberculosis in vitro and in tuberculosis-infected macrophages. They provide strong protection in tuberculosis-infected mice and have low toxicity. With some representatives of this class achieving early peak plasma concentrations approximately three orders of magnitude above minimum inhibitory concentration, they may serve as tools for improving our understanding of INH-based treatment modalities, particularly for those patients chronically underdosed in conventional INH therapy.
Texto completo:
1
Bases de datos:
MEDLINE
Métodos Terapéuticos y Terapias MTCI:
Plantas_medicinales
Asunto principal:
Bases de Schiff
/
Tuberculosis
/
Isoniazida
/
Mycobacterium tuberculosis
/
Antituberculosos
Idioma:
En
Revista:
Eur J Med Chem
Año:
2009
Tipo del documento:
Article
País de afiliación:
Estados Unidos