Document 0008
 DOCN  M9590008
 TI    Differential activities of
       1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives against
       different human immunodeficiency virus type 1 mutant strains.
 DT    9509
 AU    Balzarini J; Baba M; De Clercq E; Rega Institute for Medical Research,
       Katholieke Universiteit; Leuven, Belgium.
 SO    Antimicrob Agents Chemother. 1995 Apr;39(4):998-1002. Unique Identifier
       : AIDSLINE MED/95305568
 AB    A series of 23 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine
       derivatives that were highly potent inhibitors of wild-type human
       immunodeficiency virus type 1 strain IIIB (HIV-1/IIIB) replication in
       CEM cells were evaluated against a panel of HIV-1 mutant strains
       containing the replacement of leucine by isoleucine at position 100
       (100-Leu-->Ile), 103-Lys-->Asn, 106-Val-->Ala, 138-Glu-->Lys,
       181-Tyr-->Cys, 181-Tyr-->Ile, or 188-Tyr-->His in their reverse
       transcriptase (RT). A different structure-antiviral activity
       relationship was found, depending on the nature of the mutated amino
       acid in the HIV-1 RT. The results show that
       5-ethyl-1-ethoxymethyl-6-(3,5-dimethylbenzyl)uracil,
       5-ethyl-1-ethoxymethyl-6-(3,5-dimethylphenylthio)uracil, and
       5-ethyl-1-ethoxymethyl-6-(3,5-dimethylphenylthio)-2-thiouracil remain
       active against the majority of viruses containing single mutations which
       confer resistance to nonnucleoside RT inhibitors.
 DE    Antiviral Agents/*PHARMACOLOGY  HIV-1/*DRUG EFFECTS  Mutation  Reverse
       Transcriptase/ANTAGONISTS & INHIB  Structure-Activity Relationship
       Support, Non-U.S. Gov't  Thymine/*ANALOGS & DERIVATIVES/PHARMACOLOGY
       JOURNAL ARTICLE

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