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苯并咪唑衍生物的治疗潜力:一个特权支架的批判性评价。

A Critical Review on Therapeutic Potential of Benzimidazole Derivatives: A Privileged Scaffold.

机构信息

Department of Pharmaceutical Chemistry, C.L. Baid Metha College of Pharmacy, Dr. M.G.R. Medical University, Thoraipakkam, Chennai-600097, Tamil Nadu, lndia.

Department of Pharmaceutical Sciences, School of Pharmacy, Sathyabama Institute of Science and Technology, Chennai, lndia.

出版信息

Med Chem. 2024;20(3):311-351. doi: 10.2174/0115734064253813231025093707.

DOI:10.2174/0115734064253813231025093707
PMID:37946342
Abstract

Benzimidazole nucleus is a predominant heterocycle displaying a wide spectrum of pharmacological activities. The privileged nature of the benzimidazole scaffold has been revealed by its presence in most small molecule drugs and in its ability to bind multiple receptors with high affinity. A literature review of the scaffold reveals several instances where structural modifications of the benzimidazole core have resulted in high-affinity lead compounds against a variety of biological targets. Hence, this structural moiety offers opportunities to discover novel, better, safe and highly potent biological agents. The goal of the present review is to compile the medicinal properties of benzimidazole derivatives with a focus on SAR (Structure-Activity Relationships).

摘要

苯并咪唑核是一种主要的杂环,具有广泛的药理活性。苯并咪唑支架的特权性质已经通过它在大多数小分子药物中的存在以及它能够与多个受体高亲和力结合的能力得到了揭示。对支架的文献综述揭示了苯并咪唑核心的结构修饰导致了针对各种生物靶标的高亲和力先导化合物的几种情况。因此,该结构部分为发现新型、更好、安全和高效的生物制剂提供了机会。本综述的目的是编译苯并咪唑衍生物的药用性质,重点是 SAR(构效关系)。

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Front Pharmacol. 2021 Nov 3;12:762807. doi: 10.3389/fphar.2021.762807. eCollection 2021.
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Synthesis and fungicidal activity of novel benzimidazole derivatives bearing pyrimidine-thioether moiety against Botrytis cinerea.新型含嘧啶硫醚结构的苯并咪唑衍生物的合成及其对灰葡萄孢的抑菌活性。
Pest Manag Sci. 2021 Dec;77(12):5529-5536. doi: 10.1002/ps.6593. Epub 2021 Aug 26.
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Design, synthesis, in vitro and in vivo anti-respiratory syncytial virus (RSV) activity of novel oxizine fused benzimidazole derivatives.
Biological assessments of novel ultrasound-synthesized 2-arylbenzimidazole derivatives: antiproliferative and antibacterial effects.
新型超声合成的2-芳基苯并咪唑衍生物的生物学评估:抗增殖和抗菌作用。
RSC Med Chem. 2025 Apr 30. doi: 10.1039/d5md00106d.
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Eur J Med Chem. 2021 Jan 15;210:112964. doi: 10.1016/j.ejmech.2020.112964. Epub 2020 Oct 24.
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