杂环嘧啶衍生物作为有前途的抗菌剂。

IF 6 2区 医学 Q1 CHEMISTRY, MEDICINAL European Journal of Medicinal Chemistry Pub Date : 2023-11-05 DOI:10.1016/j.ejmech.2023.115701
Kainat Ahmed , M Iqbal Choudhary , Rahman Shah Zaib Saleem
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引用次数: 5

摘要

抗生素耐药性是一个日益严重的公共卫生问题。在探索耐药性的潜在机制的同时,需要扩大药物库。这就要求开发具有抗菌性能的新化合物。嘧啶核的功能化容易产生结构不同的化合物文库,这使嘧啶成为鉴定抗菌作用的特殊结构。嘧啶衍生物的活性可归因于与主核连接的各种亚基,特别是在C-2、C-4或C-6处。特别地,连接到嘧啶核的C-2的NH2的存在已被证明增强了对致病性革兰氏阳性菌和革兰氏阴性菌的抗菌活性。合成此类化合物所用合成路线的多样性、已报道的生物活性以及开发新型抗菌剂的日益增长的需求,值得对含嘧啶化合物的合成和抗菌活性的最新报道进行综述。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Heterocyclic pyrimidine derivatives as promising antibacterial agents

Antibiotic resistance is a growing public health concern. The quest to understand the underlying mechanisms of drug resistance needs to be accompanied by an expanded arsenal of drugs. This calls for the development of new compounds with anti-bacterial properties. The ease of functionalization of the pyrimidine core, to produce structurally distinct compound libraries, has made pyrimidine a privileged structure for identifying anti-bacterial hits. The activity of pyrimidine derivatives can be attributed to the various subunits linked with the main core, especially at C-2 or C-4 or C-6. Particularly, presence of NH2 attached to C-2 of the pyrimidine nucleus has been shown to enhance the anti-bacterial activity against pathogenic Gram-positive and Gram-negative bacteria. The diversity of synthetic routes used for the synthesis of such compounds, the reported biological activities, and a growing need to develop novel anti-bacterial agents warrant a review that presents recent reports on the synthesis and anti-bacterial activities of pyrimidine-containing compounds.

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来源期刊
CiteScore
11.70
自引率
9.00%
发文量
863
审稿时长
29 days
期刊介绍: The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.
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