Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: Part 1

We investigated proinflammatory cytokine TNFα production inhibitors in order to develop novel anti-inflammatory agents. According to the results, we found that 17, a pyrrole derivative possessing a tetrahydropyridine group at the β-position, showed potent inhibitory activity in vitro (inhibition of lipopolysaccharide (LPS) induced TNFα production in human whole blood, IC50 = 1.86 μM) and in vivo (inhibition of LPS induced TNFα production in mice, ID50 = 5.98 mg/kg).

Graphical abstractThe synthesis of the proinflammatory cytokine inhibitor 17 (TNFα ID50 = 5.98 mg/kg) is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide