N-(FUNCTIONALIZED ALKYL) DERIVATIVES OF 6-AMINOPENICILLANIC ACID: A NEW SERIES OF SPECIFIC INHIBITORS OF β-LACTAMASE FROM ENTEROBACTER CLOACAE P99

Abstract

Eight of nine new N-alkylaminopenicillanic acids (7a-c, e-j), prepared via efficient direct monoalkylation reactions, were found to be specific inhibitors of cephalosporinase P99 with IC₅₀≤4 mg/liter, while representative corresponding S-oxidized derivatives were less active.