Alcaide Anna, Trapero Ana, Pérez Yolanda, Llebaria Amadeu
Medicinal Chemistry Laboratory (MedChemLab), Departament de Química Biomèdica, Institut de Química Avançada de Catalunya (IQAC-CSIC), Jordi Girona 18-26, Barcelona, 08034, Spain.
Org Biomol Chem. 2015 May 28;13(20):5690-7. doi: 10.1039/c5ob00532a. Epub 2015 Apr 21.
A new type of galactose mimetics has been synthesized following a straightforward synthetic approach based on cyclohexene olefin aziridination reactions directed by hydroxyl substituents. These enantiomerically pure galacto-configured N-aminoaziridines are potent irreversible inhibitors of Aspergillus oryzae and Escherichia coliβ-galactosidases.
一种新型的半乳糖模拟物已通过一种基于羟基取代基导向的环己烯烯烃氮杂环丙烷化反应的直接合成方法合成出来。这些对映体纯的半乳糖构型的N-氨基氮杂环丙烷是米曲霉和大肠杆菌β-半乳糖苷酶的强效不可逆抑制剂。