Acute and chronic anti-inflammatory evaluation of imidazo[1,2-a]pyridine carboxylic acid derivatives and docking analysis
A docking analysis performed on four selected imidazo[1,2- a ]pyridine carboxylic acid derivatives indicated the binding of these to enzymes COX-1 and COX-2 active pockets. An in vitro analysis showed that compound 3-amino imidazo[1,2- a ]pyridine-2-carboxylic acid ( 5 ) preferentially inhibited COX...
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Veröffentlicht in: | Medicinal chemistry research 2012-11, Vol.21 (11), p.3491-3498 |
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Hauptverfasser: | , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | A docking analysis performed on four selected imidazo[1,2-
a
]pyridine carboxylic acid derivatives indicated the binding of these to enzymes COX-1 and COX-2 active pockets. An in vitro analysis showed that compound 3-amino imidazo[1,2-
a
]pyridine-2-carboxylic acid (
5
) preferentially inhibited COX-2. The compounds (10 mg/kg) were evaluated in relation to a potential acute and chronic anti-inflammatory activity. Compound (
5
) and imidazo[1,2-
a
]pyridine-2-carboxylic acid (
2
) inhibited the edema produced by carrageenan more efficiently than indomethacin. Chronic anti-inflammatory activity was found in derivative (
5
) and indomethacin-treated groups in the granuloma model, the compound (
2
) and nitro-acid (
4
) had only a fair activity. Compound (
2
), nitro-carboxylate (
3
), and (
5
) did not produce gastroduodenal damage. |
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ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-011-9870-3 |