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.

2-氮杂环丁酮，一种参与研究的β-内酰胺四元杂环化合物，旨在评估具有有趣生物活性的新产品。这些化合物据报道具有抗微生物和抗真菌活性。成功引入氨曲南作为头孢菌素酶的有效抑制剂，而依泽替米贝作为胆固醇吸收抑制剂被证明具有2-氮杂环丁酮部分的潜力。随后，2-氮杂环丁酮被强调为一种基于有效机理的几种酶的抑制剂，例如人类胰蛋白酶，糜酶，凝血酶，白细胞弹性蛋白酶，人巨细胞病毒蛋白酶和丝氨酸蛋白酶。还已知这些衍生物具有抗结核，抗炎，抗肿瘤，抗HIV，抗帕金森病，抗糖尿病和血管加压素V1a拮抗剂的活性。