Suppr超能文献

二氢嘧啶酮骨架作为合成特性和各种治疗靶点的有前景核心:综述

Dihydropyrimidinones Scaffold as a Promising Nucleus for Synthetic Profile and Various Therapeutic Targets: A Review.

作者信息

Khasimbi Shaik, Ali Faraat, Manda Kiran, Sharma Anjali, Chauhan Garima, Wakode Sharad

机构信息

Department of Pharmaceutical Chemistry, Delhi Institute of Pharmaceutical Sciences and Research (DIPSAR), DPSRU, Sector-3, Pushp Vihar, New Delhi, India.

Laboratory Services, Botswana Medicines Regulatory Authority, Gaborone, Botswana.

出版信息

Curr Org Synth. 2021;18(3):270-293. doi: 10.2174/1570179417666201207215710.

Abstract

BACKGROUND

This review elaborates the updated synthetic and pharmacological approaches of a known group of dihydropyrimidinones/thiones from the multi-component reaction like Biginelli reaction, which was named Pietro Biginelli in 1891. This review consists of the reaction of an aromatic aldehyde, urea and ethyl acetoacetate leading to dihydropyrimidinone/thione. Currently, the scientific movement to develop economically viable green methods using compounds that are reusable, non-volatile, easily obtained, etc. Objective: This review covers the recent synthesis and pharmacological advancement of dihydropyrimidinones/ thiones moiety, along with covering the structure-activity relationship of the most potent compounds, which may prove to become better, more efficacious and safer agents. Thus, this review may help the researchers in drug designing and development of new Dihydropyrimidinones entities.

CONCLUSION

This review focuses on the wide application of dihydropyrimidinone/thione review reports the design, synthesis and pharmacological activities of nitrogen-sulphur containing dihydropyrimidinone moiety by using multi-component reaction. Dihydropyrimidinones (DHPM) pharmacophore is an important heterocyclic ring in medicinal chemistry. It is derived from multi-component reactions, "Biginelli reaction" and plays a critical role as anticancer, antioxidant, antimicrobial, anti-inflammatory, anti-HIV-1, antimalarial, anti-inflammatory, antihypertensive and anti-tubercular agents. Exhaustive research has led to its vast biological profile, with a wide range of therapeutic application.

摘要

背景

本综述阐述了一类已知的二氢嘧啶酮/硫酮的最新合成方法和药理方法,这类化合物可通过多组分反应(如1891年以彼得罗·比吉内利命名的比吉内利反应)制得。该反应由芳香醛、尿素和乙酰乙酸乙酯反应生成二氢嘧啶酮/硫酮。目前,科学界正致力于开发经济可行的绿色方法,使用可重复使用、不挥发、易于获得等特性的化合物。目的:本综述涵盖了二氢嘧啶酮/硫酮部分的最新合成及药理进展,同时阐述了最具活性化合物的构效关系,这些化合物可能会成为更好、更有效且更安全的药物。因此,本综述可能有助于研究人员进行新型二氢嘧啶酮实体的药物设计与开发。

结论

本综述重点关注二氢嘧啶酮/硫酮的广泛应用,报道了通过多组分反应设计、合成含氮硫二氢嘧啶酮部分及其药理活性。二氢嘧啶酮(DHPM)药效团是药物化学中一个重要的杂环。它源自多组分反应“比吉内利反应”,在作为抗癌、抗氧化、抗菌、抗炎、抗HIV-1、抗疟疾、抗炎、抗高血压和抗结核药物方面发挥着关键作用。详尽的研究揭示了其广泛的生物学特性及广泛的治疗应用。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验