TY - JOUR
T1 - Acute and chronic anti-inflammatory evaluation of imidazo[1,2-A]pyridine carboxylic acid derivatives and docking analysis
AU - Márquez-Flores, Yazmín K.
AU - Campos-Aldrete, Ma Elena
AU - Sagado-Zamora, Héctor
AU - Correa-Basurto, José
AU - Meléndez-Camargo, Ma Estela
N1 - Funding Information:
Acknowledgment This study was partially supported by the Sec-retaría de Investigación y Posgrado-IPN and Conacyt (México) through grant No 49937, 91426, and 62488. One of us, Y. Márquez-Flores acknowledges Conacyt Doctoral Scholarship 202140.
PY - 2012/11
Y1 - 2012/11
N2 - 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.
AB - 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.
KW - Anti-inflammatory
KW - Carrageenan model
KW - Cyclooxygenase
KW - Docking
KW - Granuloma model
KW - Imidazo[1,2-A]pyridine
UR - http://www.scopus.com/inward/record.url?scp=84871457855&partnerID=8YFLogxK
U2 - 10.1007/s00044-011-9870-3
DO - 10.1007/s00044-011-9870-3
M3 - Artículo
SN - 1054-2523
VL - 21
SP - 3491
EP - 3498
JO - Medicinal Chemistry Research
JF - Medicinal Chemistry Research
IS - 11
ER -