Design and Synthesis of Novel 1-hydroxy-2,4,5-triaryl Imidazole Derivatives as Anti-cytokine Agents
| Author | Zahra Haghighijoo | en |
| Author | Omidreza Firuzi | en |
| Author | Savis Meili | en |
| Author | Najmeh Edraki | en |
| Author | Mehdi Khoshneviszadeh | en |
| Author | Ramin Miri | en |
| Issued Date | 2020-01-31 | en |
| Abstract | Among recent advances in the identification of anti-inflammation agents, anti-cytokines (like Interleukin-1), related to p38 MAPK families play an important role; Here in we designed new effective and low toxic anti-cytokine agents based on 1-hydroxy-2,4,5-triaryl imidazole derivatives. The reaction of oximoinoketone intermediate with ten different aromatic aldehyde and ammonium acetate in refluxing acetic acid condition give imidazole derived product, the IL-1β inhibitory assay were performed on Human PBMCs (peripheral blood mononuclear cells) using an enzyme-linked immunosorbent assay (ELISA) kit and then in computational part the binding mode of the best compound was accomplished by docking in Crystal structure of p38 MAP kinase (PDB ID: 1A9U) compared with SB202190 as standard drug. All compounds were synthesized and evaluated in biological assay showing the inhibitory activity from 28% to 82% compared to SB202190 and binding mode analysis revealed that the hydrogen-bond interactions with residues (Met109, Val30) were key point in inhibitor binding. Compound 5g clearly proved the best inhibitory action and could be further utilized for designing newer anti-cytokine agents and p38α MAP kinase potentially inhibitory action. | en |
| DOI | https://doi.org/10.22037/ijpr.2019.1100909 | en |
| Keyword | Anti-cytokine | en |
| Keyword | IL-1β | en |
| Keyword | Imidazole inhibitor | en |
| Keyword | Inflammation | en |
| Keyword | Interleukin | en |
| Keyword | P38 MAPK | en |
| Publisher | Brieflands | en |
| Title | Design and Synthesis of Novel 1-hydroxy-2,4,5-triaryl Imidazole Derivatives as Anti-cytokine Agents | en |
| Type | Original Article | en |
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