2-(2-hydroxy-4-methylphenyl)aminothiazole hydrochloride as a dual inhibitor of cyclooxygenase/lipoxygenase and a free radical scavenger. 1st communication: in vitro studies.
2-(2-Hydroxy-4-methylphenyl)aminothiazole hydrochloride (CBS-113 A) inhibits cyclooxygenase in platelets and 5-lipoxygenase in leukocytes at micromolar concentrations. On the other hand the drug is a potent scavenger of oxygen-derived free radicals. Moreover and possibly consequently, CBS-113 A inhibits the oxygen burst of stimulated leukocytes and the release of an interleukin 1-like compound from vascular endothelial cells in culture. These properties could lead to another activity of therapeutic interest in comparison with anti-inflammatory drugs already available.
Bonne
C
C
Centre de Recherches, Laboratoire Chauvin, Montpellier, France.
Muller
A
A
Latour
E
E
Tissie
G
G
Emerit
I
I
Modat
G
G
Dornand
J
J
Roch
M
M
Giroud
J P
JP
Griswold
D E
DE
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000097:blood; D001792:Blood Platelets / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D002478:Cells, Cultured; D002869:Chromosome Aberrations; D016861:Cyclooxygenase Inhibitors; D005609:Free Radicals; D006801:Humans; D066298:In Vitro Techniques; D015289:Leukotrienes / Q000096:biosynthesis / Q000097:blood; D015227:Lipid Peroxidation / Q000187:drug effects; D016859:Lipoxygenase Inhibitors; D010101:Oxygen Consumption / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001095:Arachidonic Acids; D016861:Cyclooxygenase Inhibitors; D005609:Free Radicals; D015289:Leukotrienes; D016859:Lipoxygenase Inhibitors; D013844:Thiazoles; C062488:2-(2-hydroxy-4-methylphenyl)aminothiazole; D016718:Arachidonic Acid; D013755:Tetradecanoylphorbol Acetate