Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Juliana Ruiz-Caro, Aravind Basavapathruni, Joseph T. Kim, Christopher M. Bailey, Ligong Wang, Karen S. Anderson, Andrew D. Hamilton, William L. Jorgensen

Research output: Contribution to journalArticle

Abstract

Following computational analyses, potential non-nucleoside inhibitors of HIV-1 reverse transcriptase have been pursued through synthesis and assaying for anti-viral activity. The general class Het-NH-Ph-U has been considered, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Results for compounds with Het = 2-thiazoyl and 2-pyrimidinyl are the focus of this report.

Original languageEnglish (US)
Pages (from-to)668-671
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number3
DOIs
StatePublished - Feb 1 2006

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Keywords

  • Anti-HIV drug
  • Computer-aided drug design
  • Diarylamine
  • NNRTI
  • Pyrimidinylamine
  • Thiazoylamine

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Ruiz-Caro, J., Basavapathruni, A., Kim, J. T., Bailey, C. M., Wang, L., Anderson, K. S., Hamilton, A. D., & Jorgensen, W. L. (2006). Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase. Bioorganic and Medicinal Chemistry Letters, 16(3), 668-671. https://doi.org/10.1016/j.bmcl.2005.10.037