Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 2.
Basic Information
ID: ALA1156222
Journal: Bioorg Med Chem Lett
Title: Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 2.
Authors: Nakao A, Ohkawa N, Nagasaki T, Kagari T, Doi H, Shimozato T, Ushiyama S, Aoki K.
Abstract: We previously reported a novel pyrrole derivative 1 which possesses a tetrahydropyridine group at the beta-position with a proinflammatory cytokine TNFalpha production inhibitor. Herein, we report the synthesis and biological activity of N- and alpha-position substituted tetrahydropyridine derivatives. In this series, we found that compound 3o showed good inhibitory activity in vitro (inhibition of lipopolysaccharide (LPS)-induced TNFalpha production in human whole blood, IC(50)=0.44 microM) and compound 3i demonstrated potent inhibitory activity in vivo (inhibition of LPS-induced TNFalpha production in mice, ID(50)=1.42 mg/kg).
CiteXplore: 20346666
DOI: 10.1016/j.bmcl.2010.03.022
Patent ID: ┄