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Multitarget Drugs: Synthesis and Preliminary Pharmacological Characterization of Zileuton Analogues Endowed with Dual 5‐LO Inhibitor and NO‐Dependent Activities
Author(s) -
Boschi Donatella,
Giorgis Marta,
Cena Clara,
Talniya Naveen Chandra,
Di Stilo Antonella,
Morini Giuseppina,
Coruzzi Gabriella,
Guaita Elena,
Fruttero Roberta,
Gasco Alberto
Publication year - 2010
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000198
Subject(s) - zileuton , chemistry , pharmacology , mechanism of action , leukotriene , smooth muscle , medicine , arachidonate 5 lipoxygenase , biochemistry , in vitro , arachidonic acid , enzyme , asthma
Multitarget drugs: The title compounds represent the first class of dual‐action drugs with 5‐LO inhibition and NO‐dependent activities. They block leukotriene B 4 production with potencies near that of zileuton and are capable of relaxing rat tracheal rings and rat aorta strips through a NO‐mediated mechanism. Some compounds also show anti‐inflammatory activity in carrageenan‐ induced rat paw edema.