Development of β-lactams since 1986: Commentary on The discovery of penicillin and cephalosporins by Sydney Selwyn

The discoveries of penicillins and cephalosporins enabled the treatment of communicative diseases. The β-lactam ring and the side chain make drugs that are analogs of the D-Ala-D-Ala fragment involved in cross binding of the cell wall in bacteria. Acylation of the active site thus prevents cell wall formation in bacteria. The natural antibiotics have been optimized to enable oral absorption. With the introduction of side chains, drugs have been obtained to treat diseases caused by β-lactamase-producing bacteria. Several later generations of penicillins and cephalosporins have led to the treatment of a broader range of communicative infections. Besides the penicillins and the cephalosporins, other β-lactams have been developed. β-lactamase inhibitors have also been introduced to treat infections with resistant bacteria. Unfortunately, discoveries of very resistant bacteria demand even better drugs to prevent serious epidemics. The expected profit from developing new antibiotics does not match the expense involved in drug development. Consequently, many pharmaceutical companies have been discouraged from developing such drugs.