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

Author:

Zhang Lei123,Yang Xinliang4,Yi Rui5,Wu Siming123,Li Qianbin123,Hu Gaoyun123,Chen Zhuo123ORCID

Affiliation:

1. Department of Medicinal Chemistry, Xiangya School of Pharmaceutical Sciences Central South University Changsha China

2. Hunan Key Laboratory of Organ Fibrosis Changsha Hunan China

3. Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases Changsha Hunan China

4. Department of Pharmacy Yueyang Central Hospital Yueyang Hunan China

5. Department of Pharmacy The First Affiliated Hospital of Hunan University of Medicine Huaihua Hunan China

Abstract

ABSTRACTNADPH 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.

Funder

Natural Science Foundation of Hunan Province

National Natural Science Foundation of China

Publisher

Wiley

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