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金属促进杂环化:应对大流行危机的杂合方法。

Metal-Promoted Heterocyclization: A Heterosynthetic Approach to Face a Pandemic Crisis.

机构信息

Chemistry Division, School of Science and Technology, University of Camerino, 62032 Camerino, Italy.

Laboratori Alchemia Srl, Via San Faustino, 20134 Milano, Italy.

出版信息

Molecules. 2021 Apr 29;26(9):2620. doi: 10.3390/molecules26092620.

DOI:10.3390/molecules26092620
PMID:33947170
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8124705/
Abstract

The outbreak of SARS-CoV-2 has drastically changed our everyday life and the life of scientists from all over the world. In the last year, the scientific community has faced this worldwide threat using any tool available in order to find an effective response. The recent formulation, production, and ongoing administration of vaccines represent a starting point in the battle against SARS-CoV-2, but they cannot be the only aid available. In this regard, the use of drugs capable to mitigate and fight the virus is a crucial aspect of the pharmacological strategy. Among the plethora of approved drugs, a consistent element is a heterocyclic framework inside its skeleton. Heterocycles have played a pivotal role for decades in the pharmaceutical industry due to their high bioactivity derived from anticancer, antiviral, and anti-inflammatory capabilities. In this context, the development of new performing and sustainable synthetic strategies to obtain heterocyclic molecules has become a key focus of scientists. In this review, we present the recent trends in metal-promoted heterocyclization, and we focus our attention on the construction of heterocycles associated with the skeleton of drugs targeting SARS-CoV-2 coronavirus.

摘要

SARS-CoV-2 的爆发极大地改变了我们的日常生活和全世界科学家的生活。在过去的一年中,科学界利用一切可用的工具应对这一全球性威胁,以寻找有效的应对措施。最近疫苗的配方、生产和正在进行的管理代表了对抗 SARS-CoV-2 的一个起点,但它们不能是唯一可用的手段。在这方面,使用能够减轻和对抗病毒的药物是药理学策略的一个关键方面。在众多已批准的药物中,有一个一致的元素是其骨架内的杂环框架。由于具有抗癌、抗病毒和抗炎能力,杂环化合物几十年来在制药行业中发挥了至关重要的作用。在这种情况下,开发新的、性能更高且可持续的合成策略来获得杂环分子已成为科学家们的一个重点关注领域。在这篇综述中,我们介绍了金属促进杂环化的最新趋势,并将重点放在与针对 SARS-CoV-2 冠状病毒的药物骨架相关的杂环构建上。

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Morphological Analysis of Poly(4,4'-oxydiphenylene-pyromellitimide)-Based Organic Solvent Nanofiltration Membranes Formed by the Solution Method.溶液法制备的聚(4,4'-氧二亚苯基-均苯四甲酰亚胺)基有机溶剂纳滤膜的形态分析
Membranes (Basel). 2022 Dec 7;12(12):1235. doi: 10.3390/membranes12121235.

本文引用的文献

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Anti-HIV drug repurposing against SARS-CoV-2.抗HIV药物用于治疗新型冠状病毒肺炎的研究
RSC Adv. 2020 Apr 21;10(27):15775-15783. doi: 10.1039/d0ra01899f.
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An improved synthesis of telmisartan the copper-catalyzed cyclization of -haloarylamidines.替米沙坦的改进合成方法——铜催化的卤代芳基脒环化反应。
RSC Adv. 2020 Apr 3;10(23):13717-13721. doi: 10.1039/d0ra00886a. eCollection 2020 Apr 1.
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Covid-19: New data on Oxford AstraZeneca vaccine backs 12 week dosing interval.新冠疫情:牛津大学阿斯利康疫苗的新数据支持12周的给药间隔。
BMJ. 2021 Feb 3;372:n326. doi: 10.1136/bmj.n326.
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Covid-19: New UK variant may be linked to increased death rate, early data indicate.新冠病毒:早期数据表明,英国新变种可能与死亡率上升有关。
BMJ. 2021 Jan 26;372:n230. doi: 10.1136/bmj.n230.
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Luteolin and abyssinone II as potential inhibitors of SARS-CoV-2: an in silico molecular modeling approach in battling the COVID-19 outbreak.木犀草素和阿比西酮II作为严重急性呼吸综合征冠状病毒2(SARS-CoV-2)的潜在抑制剂:应对2019冠状病毒病(COVID-19)疫情的计算机辅助分子建模方法
Bull Natl Res Cent. 2021;45(1):27. doi: 10.1186/s42269-020-00479-6. Epub 2021 Jan 20.
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The race to treat COVID-19: Potential therapeutic agents for the prevention and treatment of SARS-CoV-2.治疗 COVID-19 的竞赛:预防和治疗 SARS-CoV-2 的潜在治疗药物。
Eur J Med Chem. 2021 Mar 5;213:113157. doi: 10.1016/j.ejmech.2021.113157. Epub 2021 Jan 12.
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Reviews on Biological Activity, Clinical Trial and Synthesis Progress of Small Molecules for the Treatment of COVID-19.综述 COVID-19 小分子治疗药物的生物活性、临床试验和合成进展
Top Curr Chem (Cham). 2021 Jan 11;379(1):4. doi: 10.1007/s41061-020-00318-2.
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Covid-19: Pfizer vaccine efficacy was 52% after first dose and 95% after second dose, paper shows.论文显示,新冠疫情:辉瑞疫苗首剂接种后的效力为52%,第二剂接种后为95%。
BMJ. 2020 Dec 11;371:m4826. doi: 10.1136/bmj.m4826.
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Determination of potential inhibitors based on isatin derivatives against SARS-CoV-2 main protease (m): a molecular docking, molecular dynamics and structure-activity relationship studies.基于色酮衍生物对 SARS-CoV-2 主蛋白酶 (m) 的潜在抑制剂的测定:分子对接、分子动力学和构效关系研究。
J Biomol Struct Dyn. 2022 Apr;40(7):3110-3128. doi: 10.1080/07391102.2020.1845800. Epub 2020 Nov 17.
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Covid-19: Vaccine candidate may be more than 90% effective, interim results indicate.新冠病毒:中期结果显示,候选疫苗有效性可能超过90%。
BMJ. 2020 Nov 9;371:m4347. doi: 10.1136/bmj.m4347.