Marastoni M, Bortolotti F, Salvadori S, Tomatis R
Department of Pharmaceutical Sciences, University of Ferrara, Italy.
Arzneimittelforschung. 1998 Jun;48(6):709-12.
Two series of peptidomimetics containing 1,1-diamino-2-hydroxyethane (gSer) core structure were prepared, from amino acid starting materials, and evaluated as inhibitors of HIV-1 protease (HIV-1 Pr). Asymmetrical pseudodipeptides, Y-Xaa-gSer-Y (Y = Z, Fmoc; Xaa = Cha, Phe, Tyr, Tic) showed weak inhibitory potency (IC50 > or = 5 mumol/l), whereas the corresponding pseudotripeptides displayed a more significant HIV-1 Pr inhibition: Fmoc-Tic-gSer-Tic-Fmoc (Fmoc = fluorenylmethyloxycarbonyl, Tic = 1,2,3,4-tetradroisoquinoline-3-carboxylic acid) was the most potent compound of the series (IC50 = 385 nmol/l).
从氨基酸起始原料制备了含有1,1 - 二氨基 - 2 - 羟基乙烷（gSer）核心结构的两系列拟肽，并将其作为HIV - 1蛋白酶（HIV - 1 Pr）抑制剂进行评估。不对称假二肽Y - Xaa - gSer - Y（Y = Z、Fmoc；Xaa = Cha、Phe、Tyr、Tic）显示出较弱的抑制效力（IC50≥5 μmol/L），而相应的假三肽对HIV - 1 Pr表现出更显著的抑制作用：Fmoc - Tic - gSer - Tic - Fmoc（Fmoc = 芴甲氧羰基，Tic = 1,2,3,4 - 四氢异喹啉 - 3 - 羧酸）是该系列中最有效的化合物（IC50 = 385 nmol/L）。
