Activity of various thiocarboxanilide derivatives against wild-type and several mutant human immunodeficiency virus type 1 strains

Antiviral Res. 1995 Jun;27(3):219-36. doi: 10.1016/0166-3542(95)00006-8.


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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Benzoates / chemistry
  • Benzoates / pharmacology
  • Carboxin / analogs & derivatives*
  • Carboxin / chemistry
  • Carboxin / pharmacology
  • Cell Line
  • Drug Resistance, Microbial
  • HIV Reverse Transcriptase
  • HIV-1 / drug effects*
  • Humans
  • Mutation
  • RNA-Directed DNA Polymerase / drug effects
  • Reverse Transcriptase Inhibitors / pharmacology
  • Structure-Activity Relationship
  • Thiocarbamates / chemistry
  • Thiocarbamates / pharmacology


  • Antiviral Agents
  • Benzoates
  • NSC 615985
  • Reverse Transcriptase Inhibitors
  • Thiocarbamates
  • NSC 629243
  • Carboxin
  • HIV Reverse Transcriptase
  • RNA-Directed DNA Polymerase