Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
Bioorg Med Chem Lett
; 16(16): 4174-7, 2006 Aug 15.
Article
en En
| MEDLINE
| ID: mdl-16781149
ABSTRACT
A novel sulfanyltriazole was discovered as an HIV-1 non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Chemical modifications and molecular modeling studies were carried out to establish its SAR and understand its interactions with the enzyme. These modifications led to the identification of sulfanyltriazoles with low nanomolar potency for inhibiting HIV-1 replication and promising activities against selected NNRTI resistant mutants. These novel and potent sulfanyltriazoles could serve as advanced leads for further optimization.
Buscar en Google
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Triazoles
/
Química Farmacéutica
/
VIH-1
/
Inhibidores de la Transcriptasa Inversa
/
Fármacos Anti-VIH
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2006
Tipo del documento:
Article
País de afiliación:
Estados Unidos