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Synthesis and anti-neuroinflammatory activity of N-heterocyclic analogs based on natural biphenyl-neolignan honokiol

Authors
Yuan, YueSubedi, LalitaLim, DaesungJung, Jae-KyungKim, Sun YeouSeo, Seung-Yong
Issue Date
15-Jan-2019
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
Honokiol; Biphenyl-neolignan; Isoxazole; Pyrazole; Anti-neuroinflammatory activity
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.29, no.2, pp.329 - 333
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
29
Number
2
Start Page
329
End Page
333
URI
https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/1979
DOI
10.1016/j.bmcl.2018.11.014
ISSN
0960-894X
Abstract
Novel isoxazole and pyrazole analogs based on natural biphenyl-neolignan honokiol were synthesized and evaluated for their inhibitory activities against nitric oxide production in lipopolysaccharide-activated BV-2 microglial cells. The isoxazole skeleton was constructed via nitrile oxide cycloaddition from oxime 3 and pyrazole was generated by condensation of 4-chromone and alkylhydrazine. Among the analogs, 13b and 14a showed stronger inhibitory activities with IC50 values of 8.9 and 1.2 mu M, respectively, than honokiol.
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