喹啉（喹啉酮）衍生物作为 NADPH 氧化酶（NOX）抑制剂的设计、合成和生物学评价。

IF 3.2 4区医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Chemical Biology & Drug Design Pub Date : 2024-08-19 DOI:10.1111/cbdd.14610

Lei Zhang, Xinliang Yang, Rui Yi, Siming Wu, Qianbin Li, Gaoyun Hu, Zhuo Chen

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引用次数: 0

摘要

NADPH 氧化酶（NOXs）是人体内唯一能直接产生活性氧的酶。最近的研究表明，NOXs 是治疗糖尿病肾病（DN）的一个非常有前景的靶点。本文基于药效学策略设计了一系列喹啉（喹啉酮）衍生物，并对其进行了合成和评价。其中，19d 具有强效的抗增殖和抑制 NOXs 活性，值得进一步研究。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Design, Synthesis, and Biological Evaluation of Quinoline (Quinolinone) Derivatives as NADPH Oxidase (NOX) Inhibitors

NADPH oxidases (NOXs) are the sole enzyme in the human body that can directly produce reactive oxygen species. Recent studies have shown that NOXs is a very promising target for the treatment of diabetic nephropathy (DN). Here, a series of quinoline(quinolinone) derivatives have been designed based on pharmacophore strategy, synthesized and evaluated. Among them, 19d exhibits potent antiproliferative and NOXs inhibitory activities, and is worthy for further investigation.

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来源期刊

Chemical Biology & Drug Design 医学-生化与分子生物学

CiteScore

5.10

自引率

3.30%

发文量

164

审稿时长

4.4 months

期刊介绍： Chemical Biology & Drug Design is a peer-reviewed scientific journal that is dedicated to the advancement of innovative science, technology and medicine with a focus on the multidisciplinary fields of chemical biology and drug design. It is the aim of Chemical Biology & Drug Design to capture significant research and drug discovery that highlights new concepts, insight and new findings within the scope of chemical biology and drug design.