Nucleoside triphosphate mimicry: a sugar triazolyl nucleoside as an ATP-competitive inhibitor of B. anthracis pantothenate kinase

摘要

The synthesis of a library of nucleoside triphoshate mimetics is described where the Mg²⁺ chelated triphosphate sidechain is replaced by an uncharged methylenetriazole linked monosaccharide sidechain. The compounds have been evaluated as inhibitors of Bacillus anthracis pantothenate kinase and a competitive inhibitor has been identified with a Ki that is 3-fold lower than the Km value of ATP.