Computer-Aided Design and Synthesis of 1-{4-[(3,4-Dihydroxybenzylidene)amino]phenyl}-5-oxopyrrolidine-3-carboxylic Acid as an Nrf2 Enhancer

Shirin Kahremany; Ilana Babaev; Pinhas Hasin; Tigist Y Tamir; Tali Ben-Zur; Guy Cohen; Zhengyu Jiang; Sagiv Weintraub; Daniel Offen; Shai Rahimipour; M Ben Major; Hanoch Senderowitz; Arie Gruzman

doi:10.1002/cplu.201800155

Computer-Aided Design and Synthesis of 1-{4-[(3,4-Dihydroxybenzylidene)amino]phenyl}-5-oxopyrrolidine-3-carboxylic Acid as an Nrf2 Enhancer

Chempluschem. 2018 May;83(5):318. doi: 10.1002/cplu.201800155. Epub 2018 Apr 6.

Authors

Affiliations

¹ Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University, Ramat Gan, 5290002, Israel.
² Department of Pharmacology, and the Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA.
³ Felsenstein Medical Research Center, Sackler Faculty of Medicine, Tel-Aviv University, Rabin Medical Center-Beilinson Campus, Petah Tikva, 49100, Israel.
⁴ The Skin Research Institute, The Dead Sea & Arava Science Center, Tamar Regional Council, Dead Sea Mobile Post, 86910, Israel.
⁵ Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University Nanjing, Jiangsu, 210008, P. R. China.

PMID: 31957368
DOI: 10.1002/cplu.201800155

Abstract

Invited for this month's cover is Prof. Arie Gruzman (Bar-Ilan University) and collaborators who have developed an Nrf2 enhancer. This compound activated the Nrf2 transduction pathway and because of this the translation of dozens of antioxidant cytoprotective proteins in a dose- and time-dependent manner and protected PC-12 cells against oxidative stress. Considering the imbalance between production and elimination of oxidative species involved in the pathophysiology of many human diseases, this compound is a promising starting point for the development of novel therapeutics for the treatment of oxidative-stress-related diseases. Read the full text of the article at 10.1002/cplu.201700539.