Premium
Synthesis and Pharmacological Evaluation of Some 4‐Oxo‐quinoline‐2‐carboxylic Acid Derivatives as Anti‐inflammatory and Analgesic Agents
Author(s) -
Mazzoni Orazio,
Esposito Giovanni,
Diurno Maria Vittoria,
Brancaccio Diego,
Carotenuto Alfonso,
Grieco Paolo,
Novellino Ettore,
Filippelli Walter
Publication year - 2010
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000016
Subject(s) - analgesic , chemistry , kynurenic acid , in vivo , carboxylic acid , pharmacology , anti inflammatory , docking (animal) , quinoline , analgesic agents , chemical synthesis , biological activity , hot plate , stereochemistry , organic chemistry , biochemistry , in vitro , amino acid , medicine , tryptophan , microbiology and biotechnology , nursing , biology , mechanical engineering , engineering
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.