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

Authors :: Yuan Y
Subedi L
Lim D
Jung JK
Kim SY
Seo SY
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Jan 15; Vol. 29 (2), pp. 329-333. Date of Electronic Publication: 2018 Nov 09.
Publication Year :: 2019
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 IC <subscript>50</subscript> values of 8.9 and 1.2 µM, respectively, than honokiol.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)

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