Nucleotide competing reverse transcriptase inhibitors: discovery of a series of non-basic benzofurano[3,2-d]pyrimidin-2-one derived inhibitors.
Bioorg Med Chem Lett
; 23(9): 2781-6, 2013 May 01.
Article
em En
| MEDLINE
| ID: mdl-23545107
ABSTRACT
A HTS screen led to the identification of a benzofurano[3,2-d]pyrimidin-2-one core structure which upon further optimization resulted in 1 as a potent HIV-1 nucleotide competing reverse transcriptase inhibitor (NcRTI). Investigation of the SAR at N-1 allowed significant improvements in potency and when combined with the incorporation of heterocycles at C-8 resulted in potent analogues not requiring a basic amine to achieve antiviral activity. Additional modifications at N-1 resulted in 33 which demonstrated excellent antiviral potency and improved physicochemical properties.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirimidinonas
/
Benzofuranos
/
Inibidores da Transcriptase Reversa
/
Transcriptase Reversa do HIV
/
Nucleotídeos
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2013
Tipo de documento:
Article