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


College of Pharmacy, and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon 21936, Republic of Korea. Electronic address: [Email]


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 µM, respectively, than honokiol.


Anti-neuroinflammatory activity,Biphenyl-neolignan,Honokiol,Isoxazole,Pyrazole,