Document 0421
 DOCN  M9620421
 TI    A new series of pyridinone derivatives as potent non-nucleoside human
       immunodeficiency virus type 1 specific reverse transcriptase inhibitors.
 DT    9602
 AU    Dolle V; Fan E; Nguyen CH; Aubertin AM; Kirn A; Andreola ML; Jamieson G;
       Tarrago-Litvak L; Bisagni E; URA 1387 CNRS, Synthese Organique, Institut
       Curie, Section de; Recherche, Orsay, France.
 SO    J Med Chem. 1995 Nov 10;38(23):4679-86. Unique Identifier : AIDSLINE
       MED/96068836
 AB    4-(Arylthio)-pyridin-2(1H)-ones variously substituted in their 3-, 5-,
       and 6-positions have been synthesized as a new series of
       1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)-pyridinone
       hybrid molecules. Biological studies revealed that some of them show
       potent HIV-1 specific reverse transcriptase inhibitory properties.
       Compounds 16 and 7c, the most active ones, inhibit the replication of
       HIV-1 at 3 and 6 nM, respectively.
 DE    Antiviral Agents/*CHEMICAL SYNTHESIS/PHARMACOLOGY  HIV-1/DRUG
       EFFECTS/*ENZYMOLOGY/PHYSIOLOGY  HIV-2/ENZYMOLOGY  Kinetics  Molecular
       Structure  Pyridones/*CHEMICAL SYNTHESIS/PHARMACOLOGY  Recombinant
       Proteins/ANTAGONISTS & INHIB  Reverse Transcriptase Inhibitors/*CHEMICAL
       SYNTHESIS/PHARMACOLOGY  RNA-Directed DNA Polymerase/*METABOLISM
       Structure-Activity Relationship  Support, Non-U.S. Gov't  Virus
       Replication/DRUG EFFECTS  JOURNAL ARTICLE

       SOURCE: National Library of Medicine.  NOTICE: This material may be
       protected by Copyright Law (Title 17, U.S.Code).