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 data.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Mazzoni O,Esposito G,Diurno MV,Brancaccio D,Carotenuto A,Grieco P,Novellino E,Filippelli Wdoi
10.1002/ardp.201000016subject
Has Abstractpub_date
2010-10-01 00:00:00pages
561-9issue
10eissn
0365-6233issn
1521-4184journal_volume
343pub_type
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