The synthesis and the pharmacological activity of a series of 1-aroyl derivatives of kynurenic acid methyl ester (4-oxo-quinolin-2-carboxy methyl (KYNA) esters), structurally related to NSAID indomethacin are described. The derivatives were screened in vivo for anti-inflammatory and analgesic activities. Most of the compounds exhibited good anti-inflammatory and analgesic activities. An automatic docking of the synthesized compounds was performed using X-ray structures of COX-1 and COX-2. Docking results are in good accordance with the experimental biological data
Synthesis and pharmacological evaluation of some 4-oxo-quinoline-2-carboxylic acid derivatives as anti-inflammatory and analgesic agents / Mazzoni, O.; Esposito, G.; Diurno, M. V.; Brancaccio, D.; Carotenuto, Alfonso; Grieco, Paolo; Novellino, Ettore; Filippelli, W.. - In: ARCHIV DER PHARMAZIE. - ISSN 1521-4184. - ELETTRONICO. - 343:10(2010), pp. 561-569. [10.1002/ardp.201000016]
Synthesis and pharmacological evaluation of some 4-oxo-quinoline-2-carboxylic acid derivatives as anti-inflammatory and analgesic agents
D. Brancaccio;CAROTENUTO, ALFONSO;GRIECO, PAOLO;NOVELLINO, ETTORE;
2010
Abstract
The synthesis and the pharmacological activity of a series of 1-aroyl derivatives of kynurenic acid methyl ester (4-oxo-quinolin-2-carboxy methyl (KYNA) esters), structurally related to NSAID indomethacin are described. The derivatives were screened in vivo for anti-inflammatory and analgesic activities. Most of the compounds exhibited good anti-inflammatory and analgesic activities. An automatic docking of the synthesized compounds was performed using X-ray structures of COX-1 and COX-2. Docking results are in good accordance with the experimental biological dataI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
