Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 2.

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).

DOI: 10.1016/j.bmcl.2010.03.022

Cite this paper

@article{Nakao2010TetrahydropyridineDW, title={Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 2.}, author={Akira Nakao and Nobuyuki Ohkawa and Takayoshi Nagasaki and Takashi Kagari and Hiromi Doi and Takaichi Shimozato and Shigeru Ushiyama and Kazumasa Aoki}, journal={Bioorganic & medicinal chemistry letters}, year={2010}, volume={20 8}, pages={2435-7} }