chapter  9
74 Pages

Chemistry and Pharmacology of β-Lactam Analogs

WithAnkur Vaidya, Shweta Jain

Antimicrobial or antibacterials, drugs are the greatest contribution of the twentieth century to therapeutics. The modern era of ß-lactam antibiotics began in 1928 with the discovery of penicillin by Professor Alexander Fleming. ß-lactam antibiotics plays a center role in chemotherapy because: a potent and rapid–cidal action against bacteria in the growth phase and a very low frequency of toxic and other adverse reactions in the host. All ß-lactam antibiotics act by inhibiting bacterial cell wall synthesis. The primary bacterial resistance to the ß-lactam antibiotics is caused by the inability of the agent to penetrate to its site of action. The most important class of penicillinase is ß-lactamase that breaks the ß-lactam ring, and deactivating the molecule's antibacterial properties. The carbapenems are ß-lactam antimicrobial agents plays a critical role in our antibiotics with a broad spectrum of antibacterial activity. The carbapenems that are presently in clinical use includes imipenem-cilastatin, meropenem, ertapenem, doripenem, panipenem-ßmipron and biapenem.