title: Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 1.
abstract: We investigated proinflammatory cytokine TNFalpha 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 beta-position, showed potent inhibitory activity in vitro (inhibition of lipopolysaccharide (LPS) induced TNFalpha production in human whole blood, IC(50)=1.86 microM) and in vivo (inhibition of LPS induced TNFalpha production in mice, ID(50)=5.98 mg/kg).
authors: Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co, Ltd, 1-16-13 Kitakasai, Tokyo 134-8630, Japan. nakao.akira.g5@daiichisankyo.co.jp
authors: Akira
authors: A
authors: Nakao
authors: Nobuyuki
authors: N
authors: Ohkawa
authors: Takayoshi
authors: T
authors: Nagasaki
authors: Takashi
authors: T
authors: Kagari
authors: Hiromi
authors: H
authors: Doi
authors: Takaichi
authors: T
authors: Shimozato
authors: Shigeru
authors: S
authors: Ushiyama
authors: Kazumasa
authors: K
authors: Aoki
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000097:blood / Q000378:metabolism*
chemical_list: D000893:Anti-Inflammatory Agents; D007093:Imidazoles; D008070:Lipopolysaccharides; D011725:Pyridines; D011758:Pyrroles; D014409:Tumor Necrosis Factor-alpha; C093642:SB 203580