1. Design and synthesis of novel senkyunolide analogues as neuroprotective agents.
- Author
-
Fang Y, Wang R, Wang Q, Sun Y, Xie S, Yang Z, Li M, Jin Y, and Yang S
- Subjects
- Animals, Antioxidants chemical synthesis, Antioxidants pharmacology, Benzofurans chemical synthesis, Cell Line, Coumaric Acids pharmacology, Drug Design, Mice, Molecular Structure, Neuroprotective Agents chemical synthesis, Nitric Oxide Donors chemical synthesis, Oxadiazoles chemical synthesis, Oxidative Stress drug effects, Benzofurans pharmacology, Neuroprotective Agents pharmacology, Nitric Oxide Donors pharmacology, Oxadiazoles pharmacology
- Abstract
A class of senkyunolide analogues bearing benzofuranone fragment were designed, synthesized and evaluated for their neuroprotective effect in models of oxygen glucose deprivation (OGD) and oxidative stress. All tested compounds showed neuroprotection profile based on the cell viability assay. In particular, derivatives 1f-1i possessing furoxan-based nitric oxide releasing functionality exhibited significant biological activities in OGD models. More importantly, compound 1g containing short linker with furoxan displayed the most potent neuroprotection at the concentration of 100 μM (cell survival up to 145.2%). Besides, 1g also showed the middle level neuroprotective effect in model of oxidative stress., (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Published
- 2018
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