M. Kidwai*, P. Sapra and K.R. Bhushan Pages 195 - 215 ( 21 )
More than five decades since the Discovery of Penicillin, the chemistry and biological activity of β-lactams continue to attract the wide spread attention of research workers. Owing to high efficacy and extremely safe toxicological profile, they are agents of choice in the current therapeutic index for the bacterial infectious diseases. Tremendous efforts have been made into synthesis and structural modification of the β-lactam nucleus to increase antimicrobial activity and pharmacokinetic performance. These efforts resulted in the development of ampicillin, amoxicillin and a group of cephalosporins as clinically effective therapeutic agents. However the rapid emergence of bacterial strains resistant to most generally used members of this class of compound stimulated research for novel β-lactams, stable to β lactamase and possess high potency, broad spectrum of activity both in vitro and in vivo. The mode of action of β-lactams is to inhibit an enzyme 'transpeptidase', penicillin binding proteins, critical in the production of bacterial cell wall.