1.
Bioorg Med Chem Lett
; 19(7): 1930-4, 2009 Apr 01.
Article
in English
| MEDLINE
| ID: mdl-19269170
ABSTRACT
A new class of inhibitors of HIV-1 integrase has been optimized to provide selective and highly efficient strand transfer inhibition.
Subject(s)
HIV Integrase Inhibitors/chemical synthesis , HIV Integrase/metabolism , Pyrimidines/chemical synthesis , Animals , HIV Integrase Inhibitors/chemistry , HIV Integrase Inhibitors/pharmacokinetics , HIV-1/drug effects , Pyrimidines/chemistry , Pyrimidines/pharmacokinetics , Rats , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 16(10): 2748-52, 2006 May 15.
Article
in English
| MEDLINE
| ID: mdl-16503141
ABSTRACT
A series of aryltetrazolylacetanilides was synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors on wild-type virus and on the clinically relevant K103N mutant strain. Extensive SAR investigation led to potent compounds, with nanomolar activity on K103N, and orally bioavailable in rats.
