Syntheses of HIV-protease inhibitors having a peptide moiety which binds to GP120. NLM AIDSLINE Important note: Information in this article was accurate in 1998. The state of the art may have changed since the publication date.

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Syntheses of HIV-protease inhibitors having a peptide moiety which binds to GP120.

Chem Pharm Bull (Tokyo). 1998 Apr;46(4):697-703. Unique Identifier : AIDSLINE MED/98240208
Asagarasu A; Uchiyama T; Achiwa K; School of Pharmaceutical Sciences, University of Shizuoka, Japan.

Abstract: Some HIV-protease inhibitor derivatives having an N-carbomethoxycarbonyl-prolyl-phenylalanine benzyl ester (CPF) moiety as a binding site to gp120 were designed and synthesized. Almost all the compounds bearing CPF on the phenoxyacetyl group showed protease-inhibitory activity. Compounds 25a and 25b, which have the CPF moiety at the ortho- and meta-positions of the phenoxyacetyl group, respectively, had anti-HIV activity, although the others showed only protease-inhibitory activity. These results suggest that 25b binds to gp120 and inhibits HIV protease.
Keywords: *HIV Envelope Protein gp120/CHEMISTRY *HIV Protease Inhibitors/CHEMICAL SYNTHESIS *Oligopeptides/CHEMICAL SYNTHESIS *Virus Replication/DRUG EFFECTSKWDhivenvelopeproteingp120/chemistryKWDhivproteaseinhibitors/chemicalsynthesisKWDoligopeptides/chemicalsynthesisKWDvirusreplication/drugeffects
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