Recent Trends in the Design, Synthesis and Biological Exploration of β-Lactams

G.      Veinberg; I.      Potorocina; M.      Vorona

doi:10.2174/09298673113206660268

Abstract

Since the discovery of penicillin, natural and synthetic β-lactams have aroused great interest not only as sources of effective antibacterial agents but also as specific inhibitors of proteases responsible for various non-bacterial pathological processes. This interest was reflected in our review published in Current Medicinal Chemistry in 2003. The present article summarises new data published during the last decade dedicated to the design, synthesis and biological exploration of new β-lactams with anti-inflammatory, antiviral, anticancer and other activities based on the inhibition of human leukocyte elastase, porcine pancreatic elastase, tryptase, chymase, human cytomegalovirus protease, fatty acid amide hydrolase, protein phosphatase methylesterase-1, serine protease responsible for tumor proliferation, cysteine proteases, matrix metalloproteinases, human 20s proteasome, human immunodeficiency virus, cholesterol absorption, human fatty acid synthase, bacterial RNase A and Leishmania D-mannosyl phosphate transferase. Antitumor effect was achieved also by new β-lactams activating apoptosis-specific poly(ADP-ribose) polymerase or participating in DNA intercalation.

Keywords: Aza-β-lactams, β-lactams, β-sultams, bacterial RNase A, cholesterol absorption, cysteine proteases, cytomegalovirus protease, D-mannosyl phosphate transferase, DNA intercalation., fatty acid amide hydrolase, human fatty acid synthase, human immunodeficiency virus, inhibition, matrix metalloproteinases, poly(ADP-ribose) polymerase, protein phosphatase methylesterase-1, serine proteases.