A novel constrained reduced-amide inhibitor of HIV-1 protease derived from the sequential incorporation of. gamma.-turn mimetics into a model substrate

…, JF Callahan, ML Moore, TA Tomaszek Jr…

文献索引：Newlander; Callahan; Moore; Tomaszek Jr.; Huffman Journal of Medicinal Chemistry, 1993 , vol. 36, # 16 p. 2321 - 2331

全文：HTML全文

被引用次数: 48

摘要

C7 mimetics, designed to lock three amino acid residues of a peptide chain into a y-turn conformation, were introduced sequentially between the P3 to Pi positions of a model HIV-1 protease substrate I (resulting in compounds 11-IV) to probe its conformational requirements in binding to HIV-1 protease. Of these, compound IIIa with the C7 mimetic replacing Asn-Tyr- Pro, corresponding to the PZ through Pi positions of substrate, was found to be an inhibitor ...