Structure-activity relationships: biological

In the last fifty years a large number of β-lactam compounds have been produced, and our understanding of the structure-activity of β-lactams has increased to a remarkable degree. β-Lactams interfere with cell-wall synthesis by acylating enzymes — penicillin binding proteins (PBPs) — critical in the production of the bacterial cell wall. 1 The activity of β-lactam agents is also markedly influenced by the ability of a β-lactam compound to reach the PBP receptors, by the stability of the compound to attack by β-lactamases present in many microorganisms, which will acylate the β-lactam antibiotic and render it inactive, and by the interaction of entry, PBP binding, β-lactamase induction and stability.2-4