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Abstract

Synthesis of heterocylic compound has always drawn the attention of chemist over the years mainly because of their important biological properties. Particularly, the role of β-lactam which are endowed with unique structure and potent biological activity. The β-lactam heterocycles are considered as an important contribution of science to humanity since they have been constituents of living organisms, natural products, drugs and many more substances useful to mankind and society in all walks of life. Their synthesis and evaluation has always drawn the attention of biologists over the years. β-lactam, a four member heterocyclic compound involved in research aimed to evaluate new products that possess interesting biological activities. Natural and synthetic β-lactam derivatives occupy a central place among medicinally important compounds due to their diverse and interesting antibiotic activities and are still the most prescribed antibiotics used in medicine. The present review article focuses on the pharmacological profile of β-lactam with their potential activities. The ring system exhibits a wide range of activities like antimicrobial, antitubercular, anticancer, antidiabetic, tryptase and chymase inhibitory activity etc. attracting the attention of researchers. The biological profile of β-lactam reported by organic chemist is reviewed here comprehensively with examples under eleven different activities.

Selective toxicity of antibacterial agents—still a valid concept or do we miss chances and ignore risks?

“…Cefoperazone prevented α 1 -antitrypsin inactivation [160] and ceftazidime inhibited neutrophil elastase activity [161]. Additional reports are scarce although non-antibacterial lactams interacted with many mammalian targets [15,16,[162][163][164][165]. Whether this can be attributed to the marginal activities of commercially available ß-lactams, or if they have not been exploited systematically is uncertain.…”

Novel N-Substituted 3-Aryl-4-(diethoxyphosphoryl)azetidin-2-ones as Antibiotic Enhancers and Antiviral Agents in Search for a Successful Treatment of Complex Infections

“…On the other hand, the azetidinone ring is a common structural motif of a vast number of compounds possessing a wide range of other biological properties, including antimalarial [7], antitubercular [8], anti-inflammatory [9], antifungal [10], antidepressant [11] and nootropic activity [11]. Azetidinone derivatives are also known as cholesterol absorption [12,13], human tryptase [14,15] and chymase inhibitors [15,16], as well as vasopressin V1a antagonists [17]. Anticancer [18] and antiviral [15,19] activities of compounds having azetidinone skeleton have been also recognized.…”

“…Azetidinone derivatives are also known as cholesterol absorption [12,13], human tryptase [14,15] and chymase inhibitors [15,16], as well as vasopressin V1a antagonists [17]. Anticancer [18] and antiviral [15,19] activities of compounds having azetidinone skeleton have been also recognized. Thus, 4-(2-chlorophenyl)-3-methoxy-1-(methylthio)azetidin-2-one 1 (Figure 1) has been found to inhibit proliferation and induce apoptosis in human solid cell lines, including breast and prostate [20].…”