Design and synthesis of novel 1, 2-dithiolan-4-yl benzoate derivatives as PTP1B inhibitors. Issue 10 (15th May 2015)

• Record Type: Journal Article
• Authors: Chen, Jing; Gao, Li-Xin; Gong, Jing-Xu; Jiang, Cheng-Shi; Yao, Li-Gong; Li, Jing-Ya; Li, Jia; Xiao, Wei; Guo, Yue-Wei
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 10(2015)
• Page Start: 2211
• Page End: 2216
• Publication Date: 2015-05-15
• Subjects: Disulfide derivative -- PTP1B inhibitor -- Diabetes -- Selectivity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.03.060
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of novel 1, 2-dithiolan-4-yl benzoate compounds were synthesized and evaluated for in vitro PTP1B inhibitory activity. Some derivatives exhibited improved PTP1B inhibitory activity and selectivity compared to hit6a, a compound from in-house library screening inspired by marine cyclic disulfide. The preliminary SAR analysis with assistance of molecular modeling approach revealed6j (IC50 = 0.59 μM) as the most potent PTP1B inhibitor among all derivatives.