158221-95-5Relevant articles and documents
Syntheses of HIV-protease inhibitors having a peptide moiety which binds to GP120
Asagarasu, Akira,Uchiyama, Taketo,Achiwa, Kazuo
, p. 697 - 703 (2007/10/03)
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.