Evolution of anti-HIV drug candidates. Part 1: From α-Anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU)

Donald W. Ludovici, Michael J. Kukla, Philip G. Grous, Suma Krishnan, Koen Andries, Marie Pierre De Béthune, Hilde Azijn, Rudi Pauwels, Erik De Clercq, Edward Arnold, Paul A.J. Janssen

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92 Scopus citations

Abstract

Stemming from work on a previous clinical candidate, loviride, and other α-APA derivatives, a new series of potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been synthesized. The ITU analogues, which contain a unique diarylated imidoyl thiourea, are very active in inhibiting both wild-type and clinically important mutant strains of HIV-1.

Original languageEnglish (US)
Pages (from-to)2225-2228
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number17
DOIs
StatePublished - Sep 3 2001

All Science Journal Classification (ASJC) codes

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

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    Ludovici, D. W., Kukla, M. J., Grous, P. G., Krishnan, S., Andries, K., De Béthune, M. P., Azijn, H., Pauwels, R., De Clercq, E., Arnold, E., & Janssen, P. A. J. (2001). Evolution of anti-HIV drug candidates. Part 1: From α-Anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU). Bioorganic and Medicinal Chemistry Letters, 11(17), 2225-2228. https://doi.org/10.1016/S0960-894X(01)00410-3