Abstract:
:In this study, we have explored the prevention of gastric side effects such as gastric lesions and bleeding while maintaining the high analgesic and anti-inflammatory activities by the derivatization of the carboxylate moiety into amides in [5-chloro-6-(2-chloro/fluorobenzoyl)-2-benzoxazolinone-3-yl]acetic acids. We have tested the analgesic and anti-inflammatory activities of the synthesized compounds in vivo by using p-benzoquinone-induced writhing test and carrageenan-induced hind paw edema model, respectively. Compounds 3a, 3d, 3e, 3j and 3k potent analgesic and anti-inflammatory activities without gastric lesions in the tested animals. Therefore, conversion of the carboxylate moiety into certain amide derivatives generated potent analgesic and anti-inflammatory compounds while eliminating the gastrointestinal side effects. Cyclooxygenase (COX)-selectivity of the active compounds was also investigated by using in vitro human whole blood assay. Compounds 3a, 3e, 3h and 3k selective inhibition of COX-2 to some extent although the inhibitory activity was not very potent.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Banoglu E,Okçelik B,Kupeli E,Unlü S,Yeşilada E,Amat M,Caturla JF,Sahin MFdoi
10.1002/ardp.200300723keywords:
subject
Has Abstractpub_date
2003-07-01 00:00:00pages
251-7issue
4-5eissn
0365-6233issn
1521-4184journal_volume
336pub_type
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