IF 3.2 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Saraswati Sharma, Sahana Raju, Santosh Kumar Verma,  Kamal, Rameshwari Verma, Piyush Kumar Thakur, Kothanahally S. Sharath Kumar
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引用次数: 0

摘要

由 ESKAPE 类革兰氏阴性菌引起的感染给治疗带来了巨大挑战。这些细菌具有有效的外排泵,外膜中含有脂多糖以及厚度为 5-10 纳米的薄肽聚糖层。鲍曼不动杆菌(A. baumannii)是一种革兰氏阴性细菌,是造成医院和社区严重感染的重要因素,对人类健康构成重大威胁。这种细菌对几乎所有现有的抗生素都产生了抗药性,在过去的 50 年中,还没有一种新的抗菌药可用于治疗鲍曼尼氏菌感染,这凸显了开发新型抗菌药的迫切性。吡唑环独特的结构框架和适应性强的特点吸引着研究人员开发新的抗生素。本研究概述了过去十年中在含吡唑衍生物方面取得的进展,这些衍生物对各种细菌菌株具有广泛的抗菌活性。具体来说,我们讨论了各种吡唑衍生物对耐多药鲍曼不动杆菌菌株的有效性,并探讨了结构-活性关系(SAR)的各个方面。这些数据汇编可作为设计和开发基于吡唑的新小分子的绝佳平台,以靶向鲍曼不动杆菌的生长。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Pyrazoles: A Master Key to Tackle Multidrug-Resistant Acinetobacter baumannii and Its Structure Activity Relationship Studies

Pyrazoles: A Master Key to Tackle Multidrug-Resistant Acinetobacter baumannii and Its Structure Activity Relationship Studies

Infections caused by Gram-negative bacteria within the ESKAPE group pose significant treatment challenges. These bacteria feature effective efflux pumps and possess lipopolysaccharides in their outer membranes, as well as a thin peptidoglycan layer measuring 5–10 nm in thickness. Acinetobacter baumannii (A. baumannii), a Gram-negative bacterium, is a significant contributor to serious infections acquired in hospitals and communities, representing a substantial risk to human health. This bacterium has developed resistance to nearly all existing antibiotics, and in the past 50 years, no new antibacterial class has been introduced for treating A. baumannii infections, highlighting an urgent necessity for the development of new antibacterials. The unique structural framework and adaptable features of the pyrazole ring attract researchers to develop new antibiotics. The present study outlines the advancements made over the last decade in pyrazole-containing derivatives that exhibit a wide range of antibacterial activity against various bacterial strains. Specifically, we discuss the effectiveness of diverse pyrazole derivatives against multidrug-resistant A. baumannii strains and explore various aspects of the structure–activity relationship (SAR). This compilation of data could serve as an excellent platform for designing and developing new pyrazole-based small molecules to target the growth of A. baumannii.

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来源期刊
Chemical Biology & Drug Design
Chemical Biology & Drug Design 医学-生化与分子生物学
CiteScore
5.10
自引率
3.30%
发文量
164
审稿时长
4.4 months
期刊介绍: Chemical Biology & Drug Design is a peer-reviewed scientific journal that is dedicated to the advancement of innovative science, technology and medicine with a focus on the multidisciplinary fields of chemical biology and drug design. It is the aim of Chemical Biology & Drug Design to capture significant research and drug discovery that highlights new concepts, insight and new findings within the scope of chemical biology and drug design.
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