The present review focuses on the pharmacological profile of 2- azetidinones with their potential activities. The effect of the structures on the pharmacological activities has been discussed. 2-Azetidinone, a β-lactam four member heterocyclic compound is important for its antimicrobial and antifungal activity. This molecule is gift for patients with high cholesterol. 2-azetidinones were reposted as a potent mechanism based inhibitor of several enzymes like human tryptase, chymase, thrombin, leukocyte elastase, human cytomegalovirus protease and serine protease enzyme. As it has broad spectrum of activities it covers antitubercular, anti-inflammatory, antitumor, anti-HIV, antiparkinsonian, antidiabetic and vasopressin V1a antagonist activity too. 2-azetidinone and its derivaties have opened interesting area of research.
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