Molécules Fluorées et Chimie Médicinale, BioCIS UMR-CNRS 8076, IPSIT, Université Paris-Sud 11, Faculté de Pharmacie, 5 rue Jean-Baptiste Clément, 92296, Châtenay-Malabry Cedex, France.
ChemMedChem. 2010 Nov 8;5(11):1899-906. doi: 10.1002/cmdc.201000308.
Herein we describe the synthesis and HIV-1 protease (PR) inhibitory activity of 16 new peptidomimetic molecular tongs with a naphthalene scaffold. Their peptidic character was progressively decreased. Two of these molecules exhibited the best dimerization inhibition activity toward HIV-1 wild-type and multimutated ANAM-11 proteases obtained to date for this class of molecules (∼40 nM for wild-type PR and 100 nM for ANAM-11 PR). Although the peptidic character of one molecular tong was completely suppressed, the mechanism of inhibition and inhibitory potency toward both proteases were maintained.
在此，我们描述了具有萘支架的 16 种新型拟肽分子手的合成及其对 HIV-1 蛋白酶（PR）的抑制活性。它们的肽性质逐渐降低。其中两种分子对迄今为止获得的 HIV-1 野生型和多突变 ANAM-11 蛋白酶表现出最佳的二聚化抑制活性（野生型 PR 约为 40 nM，ANAM-11 PR 为 100 nM）。尽管一种分子手的肽性质完全被抑制，但对两种蛋白酶的抑制机制和抑制效力仍得以维持。
