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结构多样的杂环化合物和相关的优势骨架作为潜在的脲酶抑制剂:简要概述。

Structurally diversified heterocycles and related privileged scaffolds as potential urease inhibitors: a brief overview.

机构信息

Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.

出版信息

Arch Pharm (Weinheim). 2013 Jun;346(6):423-46. doi: 10.1002/ardp.201300041. Epub 2013 May 28.

DOI:10.1002/ardp.201300041
PMID:23712847
Abstract

Ureases have emerged as significant virulence factors implicated in the pathogenesis of many clinical conditions such as pyelonephritis, hepatic coma, peptic ulceration, and the formation of injection-induced urinary stones and stomach cancer. They have also been identified as important targets in research both for human and animal health, as well as in agriculture. Strategies based on urease inhibition are the main treatment of diseases caused by urease-producing bacteria. So, in the present context, a diverse library of chemical structures is known to possess remarkable inhibitory activities against urease enzymes. The current review article summarizes and discusses endeavours towards the developments in the burgeoning field of urease inhibition in medicinal chemistry, with an emphasis on the insights that have been gleaned into the structural features that contribute to high and promising levels of anti-urease activity.

摘要

脲酶已成为多种临床疾病发病机制中重要的毒力因子,这些疾病包括肾盂肾炎、肝昏迷、消化性溃疡以及注射诱导的尿路结石和胃癌。它们也被确定为人类和动物健康以及农业研究中的重要靶点。基于脲酶抑制的策略是治疗产脲酶细菌引起的疾病的主要方法。因此,在当前的背景下,人们已经知道,具有丰富化学结构的文库对脲酶具有显著的抑制活性。本文综述了在医学化学领域中脲酶抑制作用的发展,并对促进高抗脲酶活性的结构特征进行了重点讨论。

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