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1996-02-26
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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).