Buynak J D, Doppalapudi V R, Adam G
Department of Chemistry, Southern Methodist University, Dallas, TX 75275-0314, USA.
Bioorg Med Chem Lett. 2000 May 1;10(9):853-7. doi: 10.1016/s0960-894x(00)00098-6.
A series of 3-substituted-7-(alkylidene)cephaloporin sulfones were prepared and evaluated as inhibitors of representative class A and class C serine beta-lactamase. Appropriate substituents resulted in a 1000-fold improvement in the inhibition of the class A enzymes and a simultaneous 20-fold improvement in the inhibition of class C. These new compounds have achieved the goal of creating broad scale inhibitors in the cephalosporin series.
制备了一系列3-取代-7-(亚烷基)头孢菌素砜，并评估了它们作为代表性A类和C类丝氨酸β-内酰胺酶抑制剂的活性。合适的取代基使A类酶抑制活性提高了1000倍，同时C类酶抑制活性提高了20倍。这些新化合物实现了在头孢菌素系列中创制广谱抑制剂的目标。
