Synthesis and anti-neuroinflammatory activity of N-heterocyclic analogs based on natural biphenyl-neolignan honokiol
- Authors
- Yuan, Yue; Subedi, Lalita; Lim, Daesung; Jung, Jae-Kyung; Kim, Sun Yeou; Seo, 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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