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苯并呋喃作为一种有前途的骨架,可用于合成新型抗菌药物。

Benzofuran as a promising scaffold for the synthesis of novel antimicrobial agents.

机构信息

Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt.

出版信息

Expert Opin Drug Discov. 2022 Dec;17(12):1357-1376. doi: 10.1080/17460441.2023.2157400. Epub 2022 Dec 18.

Abstract

INTRODUCTION

The benzofuran moiety constitutes a main component of enormous biologically active natural and synthetic heterocycles. Such heterocycles have distinctive therapeutic potential and are employed in various clinical drugs. A number of publications have dealt with the synthesis and extraction of benzofuran-based heterocycles to investigate their antimicrobial potential.

AREAS COVERED

This review describes the antimicrobial activity of various natural and synthetic benzofuran scaffolds. The antimicrobial activity of benzofurans is thoroughly investigated against several bacterial (Gram-positive and Gram-negative) and fungal microorganisms compared with several reference antibiotic drugs. The effects of the electronic nature of substituents on the activity of benzofurans through SAR study were reported. This article also highlights the recent natural and synthetic benzofuran-based organic molecules between 2019-2022 that have had success in terms of their antimicrobial activity.

EXPERT OPINION

Many of the described benzofurans are promising candidates as antimicrobial agents based on their activity. Most used antibiotics target infections caused by the gram-positive pathogen . Interestingly, most of the described benzofurans are promising inhibitors against with either equipotent or more potent activity than the reference antibiotic drugs. These findings will encourage medicinal chemists to explore these new avenues for human health promotion to reduce suffering.

摘要

简介

苯并呋喃部分构成了大量具有生物活性的天然和合成杂环的主要成分。这些杂环具有独特的治疗潜力,并被应用于各种临床药物中。许多出版物都涉及苯并呋喃基杂环的合成和提取,以研究其抗菌潜力。

涵盖领域

本文描述了各种天然和合成苯并呋喃支架的抗菌活性。与几种参考抗生素药物相比,对苯并呋喃类化合物对几种细菌(革兰氏阳性和革兰氏阴性)和真菌微生物的抗菌活性进行了深入研究。通过 SAR 研究报道了取代基的电子性质对苯并呋喃类化合物活性的影响。本文还重点介绍了 2019-2022 年期间在抗菌活性方面取得成功的天然和合成苯并呋喃基有机分子。

专家意见

许多描述的苯并呋喃类化合物具有作为抗菌剂的潜力,基于它们的活性。大多数使用的抗生素针对由革兰氏阳性病原体引起的感染。有趣的是,大多数描述的苯并呋喃类化合物是有希望的抑制剂,对 具有与参考抗生素药物相当或更强的活性。这些发现将鼓励药物化学家探索这些新途径以促进人类健康,以减少痛苦。

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