Rational design and synthesis of a highly effective transition state analog inhibitor of the RTEM-1 β-lactamase

R Martin, JB Jones

Index: Martin, Richard; Bryan Jones, J. Tetrahedron Letters, 1995 , vol. 36, # 46 p. 8399 - 8402

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Citation Number: 30

Abstract

The synthesis of (1R)-1-acetamido-2-(3-carboxyphenyl) ethane boronic acid, a rationally designed transition state analog competitive inhibitor of the RTEM-1 β-lactamase from Escherichia coli, is reported Kinetic measurements show that, as designed, it is a highly effective reversible inhibitor of the β-lactamase, with an inhibition constant of 110 nM This is the most potent competitive inhibitor of a β-lactamase yet reported.