Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
J Med Chem
; 52(4): 1219-23, 2009 Feb 26.
Article
en En
| MEDLINE
| ID: mdl-19175319
ABSTRACT
A major problem associated with non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of HIV is their lack of resilience to mutations in the reverse transcriptase (RT) enzyme. Using structural overlays of the known inhibitors efavirenz and capravirine complexed in RT as a starting point, and structure-based drug design techniques, we have created a novel series of indazole NNRTIs that possess excellent metabolic stability and mutant resilience.
Texto completo:
1
Colección:
01-internacional
Asunto principal:
Inhibidores de la Transcriptasa Inversa
/
Fármacos Anti-VIH
/
Indazoles
Límite:
Humans
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2009
Tipo del documento:
Article
País de afiliación:
Reino Unido