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

Bioorganic & Medicinal Chemistry Letters
2009.0

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).

Knowledge Graph

Similar Paper

Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: Part 1
Bioorganic & Medicinal Chemistry Letters 2009.0
Synthesis and bioactivities of novel bicyclic thiophenes and 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-α (TNF-α) production
Bioorganic & Medicinal Chemistry Letters 2002.0
Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors
Bioorganic & Medicinal Chemistry Letters 2003.0
Novel Selective PDE4 Inhibitors. 3. In Vivo Antiinflammatory Activity of a New Series of N-Substituted cis-Tetra- and cis-Hexahydrophthalazinones
Journal of Medicinal Chemistry 2002.0
Substituted Xanthines, Pteridinediones, and Related Compounds as Potential Antiinflammatory Agents. Synthesis and Biological Evaluation of Inhibitors of Tumor Necrosis Factor α
Journal of Medicinal Chemistry 1996.0
The development of new triazole based inhibitors of tumor necrosis factor-α (TNF-α) production
Bioorganic & Medicinal Chemistry Letters 2003.0
Development of Orally Bioavailable Bicyclic Pyrazolones as Inhibitors of Tumor Necrosis Factor-α Production
Journal of Medicinal Chemistry 2004.0
Synthesis of new TNF-α Inhibitors and their biological properties
Bioorganic & Medicinal Chemistry Letters 1996.0
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice
Bioorganic & Medicinal Chemistry Letters 2016.0
Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNFα overproduction: Beneficial action in models of neuropathic pain and of acute lung inflammation
European Journal of Medicinal Chemistry 2018.0