The synthesis and evaluation of 6-alkylidene-2'beta-substituted penam sulfones as beta-lactamase inhibitors.

Autor: Buynak JD; Department of Chemistry, Southern Methodist University, Dallas, TX 75275-0314, USA., Rao AS, Doppalapudi VR, Adam G, Petersen PJ, Nidamarthy SD
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 1999 Jul 19; Vol. 9 (14), pp. 1997-2002.
DOI: 10.1016/s0960-894x(99)00325-x
Abstrakt: Penicillin sulfones, which structurally incorporate both a 6-position alkylidene substituent and a 2'beta substituent, have been synthesized and evaluated as inhibitors of class C and class A serine beta-lactamases. Incorporation of the 2'beta-substituent generally improves inhibitory activity. Substituents that improve transport across the bacterial cell membrane have also been incorporated.
Databáze: MEDLINE