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

…, S Krishnan, K Andries, MP de Bethune, H Azijn…

文献索引：Ludovici, Donald W.; Kukla, Michael J.; Grous, Philip G.; Krishnan, Suma; Andries, Koen; De Bethune, Marie-Pierre; Azijn, Hilde; Pauwels, Rudi; De Clercq, Erik; Arnold, Edward; Janssen, Paul A.J. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 17 p. 2225 - 2228

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被引用次数: 96

摘要

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.