Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
Bioorg Med Chem
; 23(5): 1069-81, 2015 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-25638501
ABSTRACT
In order to identify novel nonnucleoside inhibitors of HIV-1 reverse transcriptase two series of amide-containing uracil derivatives were designed as hybrids of two scaffolds of previously reported inhibitors. Subsequent biological evaluation confirmed acetamide uracil derivatives 15a-k as selective micromolar NNRTIs with a first generation-like resistance profile. Molecular modeling of the most active compounds 15c and 15i was employed to provide insight on their inhibitory properties and direct future design efforts.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Uracila
/
Inibidores da Transcriptase Reversa
/
Fármacos Anti-HIV
/
Acetanilidas
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2015
Tipo de documento:
Article
País de afiliação:
Federação Russa