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吡咯并[2,3 - ]嘧啶骨架在抗菌应用方面的最新进展:创新的合成策略、结构多样化及生物活性评估

Recent advances in the antimicrobial application of the pyrrolo[2,3-]pyrimidine scaffold: innovative synthetic strategies, structural diversification, and bioactivity evaluation.

作者信息

Sun Zhaoju, Li Ting, He Yi, Liu Hongwu, Yang Linli, Wu Zhibing, Liu Liwei, Luo Zhenbao, Zhou Xiang, Yang Song

机构信息

State Key Laboratory of Green Pesticides, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University Guiyang 550025 China

Bijie Branch of Guizhou Tobacco Company Bijie Guizhou 551700 China

出版信息

RSC Adv. 2025 Aug 26;15(36):29627-29645. doi: 10.1039/d5ra03313f. eCollection 2025 Aug 18.

Abstract

Antimicrobial resistance (AMR) has emerged as a critical global health challenge, necessitating urgent development of novel antimicrobial agents. Pyrrolo[2,3-]pyrimidine derivatives have garnered substantial research interest in pharmaceutical chemistry owing to their structural diversity, synthetic accessibility, and broad-spectrum bioactivity. This comprehensive review presents and discusses recent advancements in pyrrolo[2,3-]pyrimidine research, focusing on methodological innovations in scaffold construction. Key synthetic strategies, including [3 + 2] cycloadditions, transition metal-catalyzed couplings, and microwave-assisted ring closure techniques, are highlighted. Additionally, a thorough discussion of their antimicrobial activities is presented, encompassing antibacterial, antifungal, and antiviral effects. This review provides valuable insights into the rational design and synthesis of novel pyrrolo[2,3-]pyrimidine derivatives. These contributions may facilitate the development of new antimicrobial agents to address evolving resistance.

摘要

抗菌耐药性(AMR)已成为一项严峻的全球健康挑战,因此迫切需要开发新型抗菌药物。由于其结构多样性、合成可及性和广谱生物活性,吡咯并[2,3 - ]嘧啶衍生物在药物化学领域引起了广泛的研究兴趣。这篇综述介绍并讨论了吡咯并[2,3 - ]嘧啶研究的最新进展,重点关注骨架构建中的方法创新。突出了关键的合成策略,包括[3 + 2]环加成、过渡金属催化偶联和微波辅助环化技术。此外,还对其抗菌活性进行了全面讨论,包括抗菌、抗真菌和抗病毒作用。本综述为新型吡咯并[2,3 - ]嘧啶衍生物的合理设计与合成提供了有价值的见解。这些成果可能有助于开发新的抗菌药物以应对不断演变的耐药性问题。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39d2/12379008/ba2d0f122a95/d5ra03313f-f1.jpg

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