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功能化硝基咪唑支架的构建及其药物应用：1950 - 2021年综述

Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950-2021 Comprehensive Overview.

作者信息

Gupta Ria, Sharma Sumit, Singh Rohit, Vishwakarma Ram A, Mignani Serge, Singh Parvinder Pal

机构信息

Natural Product & Medicinal Chemistry Division, CSIR-Indian Institute of Integrative Medicine (CSIR-IIIM), Canal Road, Jammu 180001, India.

Academy of Scientific & Innovative Research, Gaziabad 201002, India.

出版信息

Pharmaceuticals (Basel). 2022 Apr 30;15(5):561. doi: 10.3390/ph15050561.

DOI:10.3390/ph15050561
PMID:35631389
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9144801/
Abstract

Nitroimidazole represents one of the most essential and unique scaffolds in drug discovery since its discovery in the 1950s. It was K. Maeda in Japan who reported in 1953 the first nitroimidazole as a natural product from with antibacterial activity, which was later identified as Azomycin (2-nitroimidazole) and remained in focus until now. This natural antibiotic was the starting point for synthesizing numerous analogs and regio-isomers, leading to several life-saving drugs and clinical candidates against a number of diseases, including infections (bacterial, viral, parasitic) and cancers, as well as imaging agents in medicine/diagnosis. In the present decade, the nitroimidazole scaffold has again been given two life-saving drugs (Delamanid and Pretomanid) used to treat MDR (multi-drug resistant) tuberculosis. Keeping in view the highly successful track-record of the nitroimidazole scaffold in providing breakthrough therapeutic drugs, this comprehensive review focuses explicitly on presenting the activity profile and synthetic chemistry of functionalized nitroimidazole (2-, 4- and 5-nitroimidazoles as well as the fused nitroimidazoles) based drugs and leads published from 1950 to 2021. The present review also presents the miscellaneous examples in each class. In addition, the mutagenic profile of nitroimidazole-based drugs and leads and derivatives is also discussed.

摘要

自20世纪50年代被发现以来，硝基咪唑一直是药物研发中最重要且独特的骨架之一。1953年，日本的前田健报道了首个具有抗菌活性的天然产物硝基咪唑，后来它被鉴定为偶氮霉素（2-硝基咪唑），至今仍是研究热点。这种天然抗生素是合成众多类似物和区域异构体的起点，催生出了多种挽救生命的药物以及针对多种疾病（包括感染性疾病（细菌、病毒、寄生虫感染）和癌症）的临床候选药物，还有医学诊断中的成像剂。在当前十年，硝基咪唑骨架又催生了两种用于治疗耐多药结核病的挽救生命的药物（地拉曼尼德和普瑞马尼德）。鉴于硝基咪唑骨架在提供突破性治疗药物方面的卓越成功记录，本综述明确聚焦于呈现1950年至2021年间已发表的基于功能化硝基咪唑（2-、4-和5-硝基咪唑以及稠合硝基咪唑）的药物和先导化合物的活性概况与合成化学。本综述还列举了各类中的其他实例。此外，还讨论了基于硝基咪唑的药物、先导化合物及衍生物的诱变概况。

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RSC Adv. 2020 May 1;10(29):17085-17093. doi: 10.1039/d0ra01662d. eCollection 2020 Apr 29.
2
Delamanid or pretomanid? A Solomonic judgement!德拉马尼还是普雷马尼？这真是一个棘手的问题！
J Antimicrob Chemother. 2022 Mar 31;77(4):880-902. doi: 10.1093/jac/dkab505.
3
Nitroaromatic Antibiotics as Nitrogen Oxide Sources.硝基芳香族抗生素作为一氧化氮供体。
Ethical bioprospecting and microbial assessments for sustainable solutions to the AMR crisis.
用于抗微生物药物耐药性危机可持续解决方案的伦理生物勘探和微生物评估。
IUBMB Life. 2025 Jan;77(1):e2931. doi: 10.1002/iub.2931.
4
Free Radical Production Induced by Nitroimidazole Compounds Lead to Cell Death in Amastigotes.硝咪唑类化合物诱导的自由基产生导致无鞭毛体细胞死亡。
Molecules. 2024 Aug 26;29(17):4041. doi: 10.3390/molecules29174041.
5
Sophisticated natural products as antibiotics.作为抗生素的复杂天然产物。
Nature. 2024 Aug;632(8023):39-49. doi: 10.1038/s41586-024-07530-w. Epub 2024 Jul 31.
Biomolecules. 2021 Feb 12;11(2):267. doi: 10.3390/biom11020267.
4
Antimicrobial Activity of 5-membered Nitroheteroaromatic Compounds beyond Nitrofurans and Nitroimidazoles: Recent Progress.五元含氮杂环类化合物的抗菌活性研究进展：超越硝基呋喃类和硝基咪唑类的研究。
Curr Med Chem. 2021;28(29):5926-5982. doi: 10.2174/0929867328666210216114838.
5
Strategies towards the synthesis of anti-tuberculosis drugs.抗结核药物的合成策略。
Org Biomol Chem. 2019 Jun 5;17(22):5428-5459. doi: 10.1039/c9ob00817a.
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ADMET modeling approaches in drug discovery.药物发现中的 ADMET 模型构建方法。
Drug Discov Today. 2019 May;24(5):1157-1165. doi: 10.1016/j.drudis.2019.03.015. Epub 2019 Mar 16.
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Fexinidazole: First Global Approval.非硝唑：全球首次获批。
Drugs. 2019 Feb;79(2):215-220. doi: 10.1007/s40265-019-1051-6.
8
New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.新型多胺类药物在急性和慢性期均比苯并咪唑更有效抗恰加斯病。
Eur J Med Chem. 2019 Feb 15;164:27-46. doi: 10.1016/j.ejmech.2018.12.034. Epub 2018 Dec 15.
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Efficacy of the hypoxia-activated prodrug evofosfamide (TH-302) in nasopharyngeal carcinoma in vitro and in vivo.缺氧激活前药依氟鸟氨酸（TH-302）在体外和体内对鼻咽癌的疗效。
Cancer Commun (Lond). 2018 May 3;38(1):15. doi: 10.1186/s40880-018-0285-0.
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Administration of Hypoxia-Activated Prodrug Evofosfamide after Conventional Adjuvant Therapy Enhances Therapeutic Outcome and Targets Cancer-Initiating Cells in Preclinical Models of Colorectal Cancer.常规辅助治疗后给予缺氧激活前药依氟鸟氨酸可提高结直肠癌临床前模型的治疗效果并靶向肿瘤起始细胞。
Clin Cancer Res. 2018 May 1;24(9):2116-2127. doi: 10.1158/1078-0432.CCR-17-1715. Epub 2018 Feb 23.