Bioorganic & medicinal chemistry

β-Ketophosphonates as β-lactamase inhibitors: Intramolecular cooperativity between the hydrophobic subsites of a class D β-lactamase

SK Perumal, SA Adediran, RF Pratt

Index: Perumal, Senthil K.; Adediran; Pratt Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 6987 - 6994

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Citation Number: 27

Abstract

A series of aryl and arylmethyl β-aryl-β-ketophosphonates have been prepared as potential β-lactamase inhibitors. These compounds, as fast, reversible, competitive inhibitors, were most effective (micromolar Ki values) against the class D OXA-1 β-lactamase but had less activity against the OXA-10 enzyme. They were also quite effective against the class C β- lactamase of Enterobacter cloacae P99 but less so against the class A TEM-2 enzyme. ...