Department of Chemistry and Chemical Engineering, SBASSE, Lahore University of Management Sciences, Sector-U, DHA, Lahore, 54792, Pakistan.
Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan.
Eur J Med Chem. 2023 Nov 5;259:115701. doi: 10.1016/j.ejmech.2023.115701. Epub 2023 Aug 5.
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.
抗生素耐药性是一个日益严重的公共卫生问题。为了理解耐药性的潜在机制，我们需要扩大药物储备。这就需要开发具有抗菌特性的新化合物。嘧啶核心易于功能化，可产生结构不同的化合物库，这使得嘧啶成为鉴定抗菌命中物的优势结构。嘧啶衍生物的活性可归因于与主核相连的各种亚基，尤其是在 C-2 或 C-4 或 C-6 位。特别是，嘧啶核 C-2 上连接的 NH2 的存在已被证明可以增强对致病性革兰氏阳性和革兰氏阴性细菌的抗菌活性。用于合成此类化合物的合成路线的多样性、已报道的生物学活性以及开发新型抗菌剂的需求不断增长，都需要对嘧啶类化合物的合成和抗菌活性的最新报道进行综述。
