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

Ludovici DW, Kukla MJ, Grous PG, Krishnan S, Andries K, De Béthune MP, Azijn H, Pauwels R, De Clercq E, Arnold E, Janssen PA
Bioorganic & medicinal chemistry letters (2001), Volume 11, Page 2225
PubMed entry

Abstract:

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

Polymerases:

HIV RT

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