1.
Bioorg Med Chem Lett
; 11(17): 2229-34, 2001 Sep 03.
Article
in English
| MEDLINE
| ID: mdl-11527704
ABSTRACT
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.
Subject(s)
Anti-HIV Agents/chemistry , Anti-HIV Agents/pharmacology , HIV Reverse Transcriptase/antagonists & inhibitors , Anti-HIV Agents/chemical synthesis , Drug Design , HIV Reverse Transcriptase/genetics , HIV-1/drug effects , HIV-1/genetics , Inhibitory Concentration 50 , Reverse Transcriptase Inhibitors/chemistry , Reverse Transcriptase Inhibitors/pharmacology , Structure-Activity Relationship , Triazines/chemistry
2.
Bioorg Med Chem Lett
; 11(17): 2235-9, 2001 Sep 03.
Article
in English
| MEDLINE
| ID: mdl-11527705
ABSTRACT
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.