Journal
ARCHIV DER PHARMAZIE
Volume 336, Issue 9, Pages 406-412Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.200300778
Keywords
2-oxo-3H-benzoxazole; pyridazinone; analgesic; anti-inflammatory; COX-1; COX-2
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In this study we describe the synthesis of two novel 4-phenyl- and 4-(2-chlorophenyl)-6-(5-chloro-2-oxo-3H-benzoxazol-7-yl)-3(2H)-pyridazinone derivatives (compounds 8 a and b) and their testing as inhibitors of cyclooxygenases (COX-1 and COX-2). Both compounds inhibited COX-1 (by 59 % and 61 % for compounds 8 a and 8 b respectively) and COX-2 (by 37 % and 28 % for compounds 8 a and 8 b respectively) at a concentration of 10 muM. Furthermore, we tested the analgesic and anti-inflammatory activities of the synthesized compounds in vivo by using the p-benzoquinone-induced writhing test and the carrageenan-induced hind paw edema model, respectively. Compounds 8 a and b showed potent analgesic and anti-inflammatory activities without causing gastric lesions in the tested animals.
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