Grzywa Renata, Oleksyszyn Józef
Division of Medicinal Chemistry and Microbiology, Faculty of Chemistry, Wrocław University of Technology, Wybrzeze Wyspiańskiego 27, 50-370 Wrocław, Poland.
Bioorg Med Chem Lett. 2008 Jul 1;18(13):3734-6. doi: 10.1016/j.bmcl.2008.05.050. Epub 2008 May 17.
OO-Di-trimethylsilyl esters of alpha-N-benzyloxycarbonylaminoalkylphosphinates (III) undergo triethylamine catalyzed addition to isothiocyanates to give after hydrolysis, a series of new alpha-aminoalkyl-(N-substituted)thiocarbamoyl-phosphinates. Thiocarbamoyl-phosphinate moiety can be included in the structures of the metalloproteinase inhibitors as the zinc-binding group and the new compounds reported here are good inhibitors of important aminopeptidase N(CD13) with IC(50) in range of 10.56-0.25 microM.
α-N-苄氧羰基氨基烷基次膦酸酯（III）的OO-二-三甲基硅烷基酯在三乙胺催化下与异硫氰酸酯加成，水解后得到一系列新的α-氨基烷基-（N-取代）硫代氨基甲酰基次膦酸酯。硫代氨基甲酰基次膦酸部分可作为锌结合基团包含在金属蛋白酶抑制剂的结构中，本文报道的新化合物是重要氨肽酶N（CD13）的良好抑制剂，IC（50）在10.56 - 0.25微摩尔范围内。
