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
Hauptverfasser: Márquez-Flores, Yazmín K., Campos-Aldrete, Ma. Elena, Salgado-Zamora, Héctor, Correa-Basurto, José, Meléndez-Camargo, Ma. Estela
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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.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-011-9870-3