       Document 0150
 DOCN  M9640150
 TI    Activity of various thiocarboxanilide derivatives against wild-type and
       several mutant human immunodeficiency virus type 1 strains.
 DT    9604
 AU    Balzarini J; Brouwer WG; Felauer EE; De Clercq E; Karlsson A; Rega
       Institute for Medical Research, Katholieke Universiteit; Leuven,
       Belgium.
 SO    Antiviral Res. 1995 Jun;27(3):219-36. Unique Identifier : AIDSLINE
       MED/96145332
 AB    A large variety of carboxanilide derivates in which the original
       oxathiin moiety present in the prototype compound UC84 was replaced by a
       non-cyclic lipophilic entity has been evaluated for their inhibitory
       effect against wild-type human immunodeficiency virus type 1
       (HIV-1/IIIB) and several mutant viruses derived thereof (i.e.
       HIV-1/138-Lys, HIV-1/181-Cys, HIV-1/106-Ala and HIV-1/100-IIe).
       Isopropoxy was the most favorable substituent resulting in molecules
       that were markedly inhibitory to the wild-type (EC50 0.004-0.04
       microgram/ml) as well as the mutant HIV-1 strains (EC50 0.06-0.75
       microgram/ml). In this respect, they proved superior to several other
       HIV-1-specific non-nucleoside reverse transcriptase inhibitors (NNRTIs)
       that are currently the subject of clinical trials. One of the most
       potent HIV-1 inhibitors among the thiocarboxanilide derivatives, namely
       UC38, selected for a mutant virus strain in which Lys at position 101
       and Gly at position 190 of the reverse transcriptase was replaced by
       Glu.
 DE    Antiviral Agents/CHEMISTRY/*PHARMACOLOGY
       Benzoates/CHEMISTRY/PHARMACOLOGY  Carboxin/*ANALOGS &
       DERIVATIVES/CHEMISTRY/PHARMACOLOGY  Cell Line  Drug Resistance,
       Microbial  Human  HIV-1/*DRUG EFFECTS  Mutation  Reverse Transcriptase
       Inhibitors/PHARMACOLOGY  RNA-Directed DNA Polymerase/DRUG EFFECTS
       Structure-Activity Relationship  Support, Non-U.S. Gov't
       Thiocarbamates/CHEMISTRY/PHARMACOLOGY  JOURNAL ARTICLE

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

