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Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of alpha-anilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase

Authors :
Pauwells, Rudi
Andries, Koen
Debyser, Zeger
Van Daele, Paul
Schols, Dominique
Stoffels, Paul
De Vreese, Karen
Woestenborghs, Robert
Vandamme, Anne-Mieke
Janssen, Cornelus G.M.
Anne, Jef
Cauwenbergh, Geert
Desmyter, Jan
Heykants, Jozef
Janssen, Marcel A.C.
De Clerq, Erik
Janssen, Paul A.J.
Source :
Proceedings of the National Academy of Sciences of the United States. March 1, 1993, Vol. 90 Issue 5, p1711, 5 p.
Publication Year :
1993

Abstract

A high-flux screen of 2,000 compounds obtained from a chemical library resulted in the identification of alpha-anilinophenylacetamide(alpha-APA) derivatives as potent inhibitors of human immunodeficiency virus type 1 (HIV-1) replication. These inhibitors apparently target the viral reverse transcriptase and are effective at nanomolar concentrations. One of thederivatives, R 89439, has good oral availability, favorable pharmacokinetics and can be easily synthesized.

Details

ISSN :
00278424
Volume :
90
Issue :
5
Database :
Gale General OneFile
Journal :
Proceedings of the National Academy of Sciences of the United States
Publication Type :
Academic Journal
Accession number :
edsgcl.13982156