Design and Synthesis of Novel Imidazopyridine Analogues and Evaluation as H+/K+-ATPase Antagonist
| Autor: | Sagar Patil, Ravindra S. Sonawane, Mrunal K. Shirsat, A.V. P atil, J.C. Hundiwale |
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| Rok vydání: | 2020 |
| Předmět: | |
| Zdroj: | Asian Journal of Chemistry. 32:2685-2692 |
| ISSN: | 0975-427X 0970-7077 |
| Popis: | CID data base were explored considering AZD0865 as standard and docked in proton pump ATPase pocket (PDB ID: 4ux2) to find out novel imidazopyridine derivatives as proton pump inhibitors. A number of compounds showed good proton pump ATPase inhibitory activity as per the molecular docking study as compared to standard compound AZD0865. The compound AZD0865showed a docking score of -7.11 and revealed the interactions with amino acids Asn 138 and Asp 137. A series of novel imidazopyridine derivatives as proton pump inhibitors were docked, synthesized and characterized by IR, NMR, CHN and MS spectral analysis. The target imidazopyridines were prepared from the intermediate substituted 2-aminonicotinic acid and 2-bromo-1-substituted ethanone. in vitro pharmacological studies explained that some compounds exhibited moderate to good proton pump ATPase inhibitory activity in comparison with the reference drugs i.e. AZD0865. Compound N-(3-(aminomethyl)benzyl)-3-(benzylamino)-2-(o-tolyl)imidazo[1,2-a]pyridine-8-carboxamide and N-(3-(aminomethyl)benzyl)-3-(benzylamino)-2-(4-ethylphenyl)imidazo[1,2-a]pyridine-8-carboxamide showed higher activities with the IC50 6.2 and 6.0 μg. Many compounds showed IC50 as weak antiulcer activity as compared to positive control AZD0865. |
| Databáze: | OpenAIRE |
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