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

2001; Elsevier BV; Volume: 11; Issue: 17 Linguagem: Inglês

10.1016/s0960-894x(01)00410-3

1464-3405

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

Biochemical and Molecular Research

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.