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2-氮杂环丁酮——各种药理活性的新特征。

2-Azetidinone--a new profile of various pharmacological activities.

机构信息

Department of Pharmacy, Barkatullah University, Bhopal 462026, Madhya Pradesh, India.

出版信息

Eur J Med Chem. 2010 Dec;45(12):5541-60. doi: 10.1016/j.ejmech.2010.09.035. Epub 2010 Sep 27.

Abstract

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.

摘要

2-氮杂环丁酮,一种β-内酰胺四元杂环化合物,参与旨在评估具有有趣生物活性的新产品的研究。这些化合物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和依泽替米贝作为胆固醇吸收抑制剂,证明了 2-氮杂环丁酮部分的潜力。随后,2-氮杂环丁酮被强调为几种酶的有效基于机制的抑制剂,如人组织蛋白酶、糜蛋白酶、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酶。这些衍生物还具有抗结核、抗炎、抗肿瘤、抗 HIV、抗帕金森病、抗糖尿病和血管加压素 V1a 拮抗剂活性。本文综述了 2-氮杂环丁酮的药理学特性及其潜在活性。

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