Bioorganic & medicinal chemistry

Design, synthesis, and evaluation of α-ketoheterocycles as class C β-lactamase inhibitors

S Kumar, AL Pearson, RF Pratt

Index: Kumar, Sanjai; Pearson, Andre L.; Pratt Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 8 p. 2035 - 2044

Full Text: HTML

Citation Number: 33

Abstract

A series of specific α-ketoheterocycles (benzoxazole, thiazole, imidazole, tetrazole, and thiazole-4-carboxylate) has been synthesized in order to assess their potential as β- lactamase inhibitors. The syntheses were achieved either by construction of the heterocycle (benzoxazole) from an appropriate α-hydroxyimidate, followed by oxidation of the alcohol, or by direct reaction of methyl phenaceturate with a lithiated heterocycle. The properties of ...