Synthesis of dipeptide-type human immunodeficiency virus (HIV) protease inhibitors with a binding unit to GP120

Article abstract of DOI:10.1248/cpb.46.867

Some dipeptide-type human immunodeficiency virus (HIV) protease inhibitors derived from KNI-102, with a N-carbomethoxycarbonylprolyl- phenylalanine benzyl ester (CPF) moiety as a binding site to gp120, were synthesized. Compounds 11a showed 7 - 100 times higher HIV protease- inhibitory activity (11a; IC₅₀ = 0.90 μg/ml, 1.1 μM) than the standard compound 3 or 4 (3; IC₅₀ = 3.7 μg/ml, 7.7 μM, 4; IC₅₀ = 75 μg/ml, 155 μM). Generally, the compounds substituted at the o-position of the phenoxyacetyl group 7a, 11a, 16a and 21a showed several times higher inhibitory activity than 3.

Full text of DOI:10.1248/cpb.46.867

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