Kainat Ahmed , M Iqbal Choudhary , Rahman Shah Zaib Saleem
{"title":"杂环嘧啶衍生物作为有前途的抗菌剂。","authors":"Kainat Ahmed , M Iqbal Choudhary , Rahman Shah Zaib Saleem","doi":"10.1016/j.ejmech.2023.115701","DOIUrl":null,"url":null,"abstract":"<div><p><span><span>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 </span>functionalization<span> 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 </span></span>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.</p></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"259 ","pages":"Article 115701"},"PeriodicalIF":6.0000,"publicationDate":"2023-11-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"5","resultStr":"{\"title\":\"Heterocyclic pyrimidine derivatives as promising antibacterial agents\",\"authors\":\"Kainat Ahmed , M Iqbal Choudhary , Rahman Shah Zaib Saleem\",\"doi\":\"10.1016/j.ejmech.2023.115701\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p><span><span>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 </span>functionalization<span> 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 </span></span>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.</p></div>\",\"PeriodicalId\":314,\"journal\":{\"name\":\"European Journal of Medicinal Chemistry\",\"volume\":\"259 \",\"pages\":\"Article 115701\"},\"PeriodicalIF\":6.0000,\"publicationDate\":\"2023-11-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"5\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Medicinal Chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0223523423006682\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0223523423006682","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
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.
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.