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  • Title: Syntheses of HIV-protease inhibitors having a peptide moiety which binds to GP120.
    Author: Asagarasu A, Uchiyama T, Achiwa K.
    Journal: Chem Pharm Bull (Tokyo); 1998 Apr; 46(4):697-703. PubMed ID: 9579045.
    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.
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