1.
Bioorg Med Chem Lett
; 11(17): 2229-34, 2001 Sep 03.
Artigo
em Inglês
| MEDLINE
| ID: mdl-11527704
RESUMO
A synthesis program directed toward improving the stability of imidoyl thiourea based non-nucleoside reverse transcriptase inhibitors (NNRTIs) led to the discovery of diaryltriazines (DATAs), a new class of potent NNRTIs. The synthesis and anti-HIV structure-activity relationship (SAR) studies of a series of DATA derivatives are described.
Assuntos
Fármacos Anti-HIV/química , Fármacos Anti-HIV/farmacologia , Transcriptase Reversa do HIV/antagonistas & inibidores , Fármacos Anti-HIV/síntese química , Desenho de Fármacos , Transcriptase Reversa do HIV/genética , HIV-1/efeitos dos fármacos , HIV-1/genética , Concentração Inibidora 50 , Inibidores da Transcriptase Reversa/química , Inibidores da Transcriptase Reversa/farmacologia , Relação Estrutura-Atividade , Triazinas/química
2.
Bioorg Med Chem Lett
; 11(17): 2235-9, 2001 Sep 03.
Artigo
em Inglês
| MEDLINE
| ID: mdl-11527705
RESUMO
The synthesis and anti-HIV-1 activity of a series of diarylpyrimidines (DAPYs) are described. Several members of this novel class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) are extremely potent against both wild-type and a panel of clinically significant single- and double-mutant strains of HIV-1.
