Antibiotic sulfonylaminocarbonyl activated beta-lactams.

摘要

This invention presents novel 2-azetidinone compounds which are useful as antibacterial agents to eradicate or control susceptible microbes of the formula <CHEM> wherein R401 and R402 are the same or different and are a) hydrogen, b) (C1-C12) alkyl c) (C2-C8) alkenyl, d) (C2-C8) alkynyl, e) (C3-C10) cycloalkyl, f) phenyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C1-C4)alkyl, and (C1-C4)alkoxy, g) benzyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C1-C4)alkyl, and (C1-C4)alkoxy, h) -CH2-O-CO-CH2-NHR420, i) -CH2-O-CO2-R430, j) -CH2F, or k) -CHF2; wherein R420 is a) hydrogen, b) -COH, or c) -CO-O-C(CH3)3; wherein R430 is (C1-C8)alkyl, -(CH2)2OC(O)NH2, -(CH2)2Cl, -(CH2)2OCH3 or -(CH2)2NHCOH; wherein R300 is an acyl group derived from a carboxylic acid; wherein R100 is an optionally substituted heterocyclic moiety.