Design, synthesis and SAR study of novel C2-pyrazolopyrimidine amides and amide isosteres as allosteric integrase inhibitors.
Bioorg Med Chem Lett
; 30(21): 127516, 2020 11 01.
Article
em En
| MEDLINE
| ID: mdl-32860982
ABSTRACT
The design, synthesis and structure-activity relationships associated with a series of C2-substituted pyrazolopyrimidines as potent allosteric inhibitors of HIV-1 integrase (ALLINIs) are described. Structural modifications to these molecules were made in order to examine the effect on potency and, for select compounds, pharmacokinetic properties. We examined a variety of C2-substituted pyrazolopyrimidines and found that the C2-amide derivatives demonstrated the most potent antiviral activity of this class against HIV-1 infection in cell culture.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirazóis
/
Pirimidinas
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Inibidores de Integrase de HIV
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Integrase de HIV
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Fármacos Anti-HIV
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Amidas
Limite:
Humans
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article