2-azetidinone, a β-lactam four member heterocyclic compound involved in research aimed to evaluate new products that possess interesting biological activities. These compounds reported for their antimicrobial and antifungal activities. Successful introduction of aztreonam as a potent inhibitor of cephalosporinase and ezetimibe as a cholesterol absorption inhibitor proved potential of 2-azetidinone moiety. Subsequently 2-azetidinones were highlighted as a potent mechanism based inhibitor of several enzymes like human tryptase, chymase, thrombin, leukocyte elastase, human cytomegalovirus protease and serine protease enzyme. These derivatives also known to possess antitubercular, anti-inflammatory, antitumor, anti-HIV, antiparkinsonian, antidiabetic and vasopressin V1a antagonist activity. The present review article focuses on the pharmacological profile of 2-azetidinones with their potential activities.
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