2. Academic Validation
  3. Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU)

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

  • Bioorg Med Chem Lett. 2001 Sep 3;11(17):2225-8. doi: 10.1016/s0960-894x(01)00410-3.
D W Ludovici 1,  M J Kukla,  P G Grous,  S Krishnan,  K Andries,  M P de Béthune,  H Azijn,  R Pauwels,  E De Clercq,  E Arnold,  P A Janssen
Affiliations

Affiliation

  • 1 Janssen Research Foundation, Welsh and McKean Roads, Spring House, PA 19477, USA.
PMID: 11527703 DOI: 10.1016/s0960-894x(01)00410-3
Abstract

Stemming from work on a previous clinical candidate, loviride, and Other alpha-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.

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