Synthesis, p38 Kinase Inhibitory and Anti-inflammatory Activity of New Substituted Benzimidazole Derivatives
| Autor: | Stefan Laufer, Ravindra Kulkarni, Achaiah Garlapati, Chandrashekhar V M |
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| Rok vydání: | 2013 |
| Předmět: |
Benzimidazole
Molecular Structure medicine.drug_class Kinase p38 mitogen-activated protein kinases Anti-Inflammatory Agents p38 Mitogen-Activated Protein Kinases In vitro Anti-inflammatory Rats Enzyme Activation Structure-Activity Relationship chemistry.chemical_compound chemistry Biochemistry In vivo Docking (molecular) Drug Design Drug Discovery medicine Animals Structure–activity relationship Benzimidazoles Enzyme Inhibitors |
| Zdroj: | Medicinal Chemistry. 9:91-99 |
| ISSN: | 1573-4064 |
| DOI: | 10.2174/157340613804488440 |
| Popis: | P38 mitogen activated protein kinases have been found to involve in the production and release of unwarranted levels of pro-inflammatory cytokines including TNFα and IL-1β in numerous inflammatory diseases. A new series of molecules, 5-substituted benzoylamino-2-substituted phenylbezimidazoles has been synthesized from 4-nitro-1, 2- diaminobenzene. The synthesized compounds were characterized by FTIR, 1HNMR and Mass. The final compounds were screened for in vitro p38 kinase inhibitory and in vivo anti-inflammatory activity. Three compounds from the series demonstrated nearly 50% inhibition of p38 kinase in the in vitro screening method at 10 μM concentration and two molecules exhibited greater than 75% inhibition of paw oedema volume during the first hour. The docking study of synthesized molecule revealed a new binding pose in ATP binding pocket. |
| Databáze: | OpenAIRE |
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