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尿酶抑制剂治疗应用的专利更新(2012-2018 年)。

A patent update on therapeutic applications of urease inhibitors (2012-2018).

机构信息

a H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences , University of Karachi , Karachi , Pakistan.

b Department of Chemistry , Forman Christian College (A Chartered University) , Lahore , Pakistan.

出版信息

Expert Opin Ther Pat. 2019 Mar;29(3):181-189. doi: 10.1080/13543776.2019.1584612. Epub 2019 Mar 6.

Abstract

INTRODUCTION

Urease is a nickel-containing metalloenzyme that is commonly found in different bacteria, plants, algae, and fungi and mediates the growth of many pathogenic bacteria in the acidic environment of the stomach. Despite the large number of molecules known to have excellent urease inhibitory activity, there is an alarming lack of urease inhibitor drugs on the market.

AREAS COVERED

This review aims to provide a comprehensive overview of the different types of molecules patented as potent urease inhibitors from the year 2012 to 2018.

EXPERT OPINION

Urease is an important target to treat urease-related bacterial infections manifesting as gastric ulcers, urinary tract infections, and kidney stones. Although many different molecules as inhibitors of urease have been reported, only a few have advanced to clinical trials. The development of new effective urease inhibitors demands new suitable lead molecules. This review covers the patents on urease inhibitors in recent years (2012-2018) with a hope to bring into focus the issue and need for availability of new urease inhibitors on the market.

摘要

简介

脲酶是一种含镍的金属酶,广泛存在于不同的细菌、植物、藻类和真菌中,介导许多致病性细菌在胃酸性环境中的生长。尽管有大量已知具有优异脲酶抑制活性的分子,但市场上严重缺乏脲酶抑制剂药物。

涵盖领域

本篇综述旨在全面概述 2012 年至 2018 年期间以强效脲酶抑制剂为特征的不同类型分子的专利情况。

专家意见

脲酶是治疗因脲酶相关细菌感染引起的胃溃疡、尿路感染和肾结石的重要靶点。尽管已经报道了许多不同的脲酶抑制剂分子,但只有少数几种进入临床试验阶段。开发新的有效的脲酶抑制剂需要新的合适的先导分子。本篇综述涵盖了近年来(2012-2018 年)脲酶抑制剂的专利情况,希望能引起人们对市场上新的脲酶抑制剂的需求和可用性的关注。

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