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
  • 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.