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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 24, 2009 - Issue 1
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Research Article

Synthesis and characterization of some new 2(3H)-benzoxazolones with analgesic and antiinflammatory activities

Nesrin Gökhan-Kelekçi Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, 06100 Sihhiye, Ankara, TurkeyCorrespondence[email protected]
,
Meriç Köksal Faculty of Pharmacy, Yeditepe University, 34755 Kayişdağı, Istanbul, Turkey
,
Songül Ünüvar Department of Pharmacology, Faculty of Pharmacy, Inönü University, 44280 Malatya, Turkey
,
Göknur Aktay Department of Pharmacology, Faculty of Pharmacy, Inönü University, 44280 Malatya, Turkey
&
Hakki Erdoğan Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, 06100 Sihhiye, Ankara, Turkey
Pages 29-37 | Received 27 Jul 2007, Accepted 08 Nov 2007, Published online: 20 Oct 2008
 
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Abstract

The synthesis, characterization and pharmacological activities of a new series of (6-difluorobenzoyl)-5-methyl-3-benzoylmethyl-2(3H)-benzoxazolone and 5-methyl-3-(2-hydroxyl-2-phenylethyl)-2(3H)-benzoxazolone are described. Antiinflammatory activity was investigated by the carrageenin-induced paw oedema test and analgesic activity by acetic acid writhing and hot plate tests in mice. Among the synthesized compounds, compound 3e 6-(2,5-difluorobenzoyl)-3-(4-bromobenzoylmethyl-2(3H)-benzoxazolone was found to be the most promising compound for analgesic activity. Reduced compounds (4a–4d) displayed considerable anti-inflammatory activity compared to the other derivatives.

Acknowledgements

This study was supported by the Hacettepe University Research Center Fund (Project number: 05 D 301002).

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