2-(2-hydroxy-4-methylphenyl)aminothiazole hydrochloride as a dual inhibitor of cyclooxygenase/lipoxygenase and a free radical scavenger. 2nd communication: anti-inflammatory activity.
The paper describes the topical anti-inflammatory activity of 2-(2-hydroxy-4-methylphenyl)aminothiazole hydrochloride (CBS-113 A), a dual inhibitor of cyclooxygenase/lipoxygenase and a potent free radical scavenger. When applied in eye drops (0.01 to 0.1% according to the model used), the drug inhibited inflammation in experimental conjunctivitis and uveitis induced by various procedures (e.g. paracentesis, endotoxin, S-antigen, albumin, Fe2+). The compound also inhibited leukocyte infiltration and histamine release when administered locally in pleural cavity with carrageenan. CBS-113 A could decrease plasma leakage induced by arachidonic acid or platelet activating factor in skin and airway, respectively. However, it was devoid of any activity when administered by systemic route. The compound appears as a potentially useful anti-inflammatory drug, in particular in ophthalmology and as an alternative to glucocorticoids, since it does not present the side effects of these steroids (e.g. worsening of herpetic keratitis).
Bonne
C
C
Centre de Recherches, Laboratoire Chauvin, Montpellier, France.
Latour
E
E
Muller
A
A
de Kozak
Y
Y
Faure
J P
JP
Malet
F
F
Colin
J
J
Tissot
M
M
Giroud
J P
JP
Maghni
K
K
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D003231:Conjunctivitis / Q000139:chemically induced / Q000188:drug therapy; D016861:Cyclooxygenase Inhibitors; D005609:Free Radicals; D006168:Guinea Pigs; D006967:Hypersensitivity / Q000188:drug therapy; D007634:Keratitis / Q000188:drug therapy; D016859:Lipoxygenase Inhibitors; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010998:Pleurisy / Q000139:chemically induced / Q000188:drug therapy; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D013844:Thiazoles / Q000494:pharmacology*; D014605:Uveitis / Q000139:chemically induced / Q000188:drug therapy
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D005609:Free Radicals; D016859:Lipoxygenase Inhibitors; D013844:Thiazoles; C062488:2-(2-hydroxy-4-methylphenyl)aminothiazole