Tetrahedron

N-Sulfonyloxy-β-lactam inhibitors for β-lactamases

A Bulychev, JR Bellettini, M O'Brien, PJ Crocker…

Index: Bulychev, Alexey; Bellettini, John R.; O'Brien, Michael; Crocker, Peter J.; Samama, Jean-Pierre; Miller, Marvin J.; Mobashery, Shahriar Tetrahedron, 2000 , vol. 56, # 31 p. 5719 - 5728

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Citation Number: 36

Abstract

Structure-function analysis with a series of N-sulfonyloxy β-lactam molecules as inhibitors of β-lactamases is reported. The best of these compounds acylate the active site of the class A TEM-1 β-lactamase from Escherichia coli rapidly, and resist deacylation. Whereas acylation of the active site of the class C β-lactamase from Enterobacter cloacae was not seen, these compounds function as competitive inhibitors of this enzyme.