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

Research output: Contribution to journalArticle

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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

Fingerprint

Anti-HIV Agents
Thiourea
loviride
Reverse Transcriptase Inhibitors
HIV-1
Derivatives

All Science Journal Classification (ASJC) codes

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

Cite this

Ludovici, D. W., Kukla, M. J., Grous, P. G., Krishnan, S., Andries, K., De Béthune, M. P., ... 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
Ludovici, Donald W. ; Kukla, Michael J. ; Grous, Philip G. ; Krishnan, Suma ; Andries, Koen ; De Béthune, Marie Pierre ; Azijn, Hilde ; Pauwels, Rudi ; De Clercq, Erik ; Arnold, Edward ; Janssen, Paul A.J. / Evolution of anti-HIV drug candidates. Part 1 : From α-Anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU). In: Bioorganic and Medicinal Chemistry Letters. 2001 ; Vol. 11, No. 17. pp. 2225-2228.
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Ludovici, DW, Kukla, MJ, Grous, PG, Krishnan, S, Andries, K, De Béthune, MP, Azijn, H, Pauwels, R, De Clercq, E, Arnold, E & Janssen, PAJ 2001, 'Evolution of anti-HIV drug candidates. Part 1: From α-Anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU)', Bioorganic and Medicinal Chemistry Letters, vol. 11, no. 17, pp. 2225-2228. https://doi.org/10.1016/S0960-894X(01)00410-3

Evolution of anti-HIV drug candidates. Part 1 : From α-Anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU). / Ludovici, Donald W.; Kukla, Michael J.; Grous, Philip G.; Krishnan, Suma; Andries, Koen; De Béthune, Marie Pierre; Azijn, Hilde; Pauwels, Rudi; De Clercq, Erik; Arnold, Edward; Janssen, Paul A.J.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 17, 03.09.2001, p. 2225-2228.

Research output: Contribution to journalArticle

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