(2,3)-(α-methylenepenams: Synthesis and in vitro activity

Abstract A series of α-methylene penicillins was synthesized and SAR were studied. The α-isomers were found to be chemically reactive and biologically active in contrast to the β-isomers. In addition, the α-isomers have broader spectrum of in vitro activity than the corresponding penicillins. Generally, the α-isomers are more active against gram-negative bacteria than the corresponding penicillins, but slightly weaker in potency towards gram-positive organisms.