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嘧啶酮衍生物的合成及生物活性研究进展。

Recent Developments on the Synthesis and Biological Activities of Fused Pyrimidinone Derivatives.

机构信息

School of Chemistry and Physics, University of Kwa-Zulu Natal, Private Bag X01, Scottsville, Durban, South Africa.

出版信息

ChemMedChem. 2021 Jul 6;16(13):2050-2067. doi: 10.1002/cmdc.202100083. Epub 2021 May 7.

Abstract

Heterocyclic compounds constitute a unique class of organic compounds endowed with a wide range of synthetic and pharmaceutical applications. Pyrimidinones and their fused analogues have received focused attention in this regard, partly due to their mimicry of nucleobases which consequently forges their interesting medicinal properties. Over the years, the medicinal chemistry research community has experienced an upsurge in articles describing the exploration of these scaffolds to develop effective therapeutic agents. Several biological activities, including antimicrobial, antiviral, anticancer, antidiabetic, anti-inflammatory, anticonvulsive, and antihistaminic, have been well documented. This minireview presents a compendium of recent developments (2017-2020) focused on the synthesis and biological activities of fused pyrimidinones. The goal is to update medicinal chemists on the therapeutic relevance of fused pyrimidinones and the molecular architecture of clinic-worthy drug candidates. A brief account of the structure-activity relationships (SAR) revealed from different biological assays is also discussed.

摘要

杂环化合物是一类具有广泛合成和药用应用的独特有机化合物。嘧啶酮及其稠合类似物在这方面受到了特别关注,部分原因是它们模拟了核苷酸碱基,从而赋予了它们有趣的药用特性。多年来,药物化学研究界发表了大量描述这些支架的探索文章,以开发有效的治疗剂。已经有多种生物活性得到了很好的记录,包括抗菌、抗病毒、抗癌、抗糖尿病、抗炎、抗惊厥和抗组胺。本文综述了 2017 年至 2020 年期间关于稠合嘧啶酮的合成和生物活性的最新进展。目的是让药物化学家了解稠合嘧啶酮的治疗相关性和有临床应用价值的候选药物的分子结构。还讨论了不同生物测定中揭示的构效关系(SAR)的简要说明。

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