Rowan Andrew S, Nicely Nathan I, Cochrane Nicola, Wlassoff Wjatschesslaw A, Claiborne Al, Hamilton Chris J
School of Chemistry and Chemical Engineering, David Keir Building, Stranmillis Road, Queen's University Belfast, Belfast, BT9 5AG.
Org Biomol Chem. 2009 Oct 7;7(19):4029-36. doi: 10.1039/b909729e. Epub 2009 Jul 27.
The synthesis of a library of nucleoside triphosphate mimetics is described where the Mg(2+) chelated triphosphate sidechain is replaced by an uncharged methylene-triazole linked monosaccharide sidechain. The compounds have been evaluated as inhibitors of Bacillus anthracis pantothenate kinase and a competitive inhibitor has been identified with a K(i) that is 3-fold lower than the K(m) value of ATP.
描述了核苷三磷酸模拟物文库的合成,其中镁离子螯合的三磷酸侧链被不带电荷的亚甲基-三唑连接的单糖侧链取代。这些化合物已被评估为炭疽芽孢杆菌泛酸激酶的抑制剂,并鉴定出一种竞争性抑制剂,其抑制常数(K(i))比ATP的米氏常数(K(m))低3倍。