beta-Lactams, being a structural motif in most widely used antibiotics, have occupied a pivotal position in medicinal chemistry for almost a century now. With the microorganisms retaliating the traditional antibiotics via beta-lactamase enzymes, the need for novel antibiotics prevails making the synthesis of newer beta-lactams ever more important. Besides their use as antibiotics, beta-lactams are increasingly being used as synthons for biologically important molecules. beta-Lactams have been found to act as cholesterol acyltransferase inhibitors, thrombin inhibitors, human cytomegalovirus protease inhibitors, matrix metalloprotease inhibitors, cysteine protease, and apoptosis inductors.
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