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Title
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Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
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Authors
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D.W.Ludovici,
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.
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Ref.
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Bioorg Med Chem Lett, 2001,
11,
2225-2228.
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PubMed id
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Abstract
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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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