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苯并咪唑的合成与构效关系:抗菌创新洞察(2018 - 2024年)

Synthesis and SARs of benzimidazoles: insights into antimicrobial innovation (2018-2024).

作者信息

Ibrahim Ahmed A, Said Eman G, AboulMagd Asmaa M, Amin Noha H, Abdel-Rahman Hamdy M

机构信息

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Nahda University in Beni-Suef (NUB) Beni-Suef 62513 Egypt

Medicinal Chemistry Department, Faculty of Pharmacy, Beni-Suef University Beni-Suef 62514 Egypt.

出版信息

RSC Adv. 2025 Jun 30;15(27):22097-22127. doi: 10.1039/d5ra00819k. eCollection 2025 Jun 23.

Abstract

Benzimidazole derivatives have garnered significant attention in medicinal chemistry owing to their versatile pharmacological properties, particularly their potent antimicrobial activity. This review comprehensively explores the advancements in the synthesis of benzimidazoles and their antimicrobial property evaluation from 2018 to 2024. Recent synthetic methodologies emphasize green chemistry approaches including solvent-free and catalyst-driven reactions, offering improved yields, selectivity, and environmental sustainability. Structural modifications, such as functionalization at positions 2 and 5/6 of the benzimidazole ring, were extensively investigated to enhance the antimicrobial efficacy against a broad spectrum of pathogens including multidrug-resistant bacterial and fungal strains. Furthermore, we elucidate the structure-activity relationships (SARs) of benzimidazole derivatives, enabling the rational design of highly potent antimicrobial agents. The mentioned period also witnessed the integration of hybrid molecules, wherein benzimidazoles were conjugated with other bioactive scaffolds to achieve synergistic antimicrobial effects.

摘要

苯并咪唑衍生物因其多样的药理特性,特别是其强大的抗菌活性,在药物化学领域备受关注。本综述全面探讨了2018年至2024年苯并咪唑类化合物的合成进展及其抗菌性能评估。近期的合成方法强调绿色化学方法,包括无溶剂和催化剂驱动的反应,可提高产率、选择性和环境可持续性。人们广泛研究了结构修饰,如在苯并咪唑环的2位和5/6位进行官能化,以增强对包括多重耐药细菌和真菌菌株在内的广泛病原体的抗菌效果。此外,我们阐明了苯并咪唑衍生物的构效关系(SARs),从而能够合理设计高效抗菌剂。在上述时期还见证了杂化分子的整合,其中苯并咪唑与其他生物活性支架共轭以实现协同抗菌效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a373/12208292/1094978e19f4/d5ra00819k-f1.jpg

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