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Molecules 2012, 17(10), 12262-12275; doi:10.3390/molecules171012262
Article

Design, Synthesis and in Vivo Anti-inflammatory Activities of 2,4-Diaryl-5-4H-imidazolone Derivatives

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, 2,3,* , 4, 3 and 3
Received: 22 August 2012; in revised form: 12 September 2012 / Accepted: 11 October 2012 / Published: 18 October 2012
(This article belongs to the Section Medicinal Chemistry)
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Abstract: A series of 2,4-diaryl-5(4H)-imidazolones were prepared and evaluated for their anti-inflammatory activities. Some selected 2,4-diaryl-5(4H)-imidazolones exhibited excellent anti-inflammatory activity in the carrageenan-induced rat paw edema model. Structure Activity Relationships within the series were studied. The substitution at the N-sulfonamide moiety by a small hydrophilic acetyl group resulted in compounds with superior in vivo anti-inflammatory properties. As expected from their COX-2 selectivity, most of the active compounds lacked gastrointestinal toxicity in vivo in rats after a 3-day treatment of 25 mg/kg/day.
Keywords: anti-inflammatory; COX-2; COX-2 inhibitors; imidazolone; oxazolone; docking; structure-based design anti-inflammatory; COX-2; COX-2 inhibitors; imidazolone; oxazolone; docking; structure-based design
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

El-Araby, M.; Omar, A.; Hassanein, H.H.; El-Helby, A.-G.; Abdel-Rahman, A.A. Design, Synthesis and in Vivo Anti-inflammatory Activities of 2,4-Diaryl-5-4H-imidazolone Derivatives. Molecules 2012, 17, 12262-12275.

AMA Style

El-Araby M, Omar A, Hassanein HH, El-Helby A-G, Abdel-Rahman AA. Design, Synthesis and in Vivo Anti-inflammatory Activities of 2,4-Diaryl-5-4H-imidazolone Derivatives. Molecules. 2012; 17(10):12262-12275.

Chicago/Turabian Style

El-Araby, Moustafa; Omar, Abdelsattar; Hassanein, Hassanein H.; El-Helby, Abdel-Ghany H.; Abdel-Rahman, Asharf A. 2012. "Design, Synthesis and in Vivo Anti-inflammatory Activities of 2,4-Diaryl-5-4H-imidazolone Derivatives." Molecules 17, no. 10: 12262-12275.



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