Discovery of boron-containing compounds as Aβ aggregation inhibitors and antioxidants for the treatment of Alzheimer's disease. Issue 11 (9th October 2018)

• Record Type: Journal Article
• Authors: Lu, Chuan-Jun; Hu, Jinhui; Wang, Zechen; Xie, Shishun; Pan, Tingting; Huang, Ling; Li, Xingshu
• Is Part Of: MedChemComm. Volume 9:Issue 11(2018)
• Page Start: 1862
• Page End: 1870
• Publication Date: 2018-10-09
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c8md00315g
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : A novel series of boron-containing compounds were designed, synthesized and evaluated as multi-target-directed ligands against Alzheimer's disease. Abstract : A novel series of boron-containing compounds were designed, synthesized and evaluated as multi-target-directed ligands against Alzheimer's disease. The biological activity results demonstrated that these compounds possessed a significant ability to inhibit self-induced Aβ aggregation (20.5–82.8%, 20 μM) and to act as potential antioxidants (oxygen radical absorbance capacity assay using fluorescein (ORAC-FL) values of 2.70–5.87). In particular, compound17h is a potential lead compound for AD therapy (IC50 = 3.41 μM for self-induced Aβ aggregation; ORAC-FL value = 4.55). Compound17h also functions as a metal chelator. These results indicated that boron-containing compounds could be new structural scaffolds for the treatment of AD.