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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

1,2
,
2,3,* , 4, 3 and 3
1 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Cairo 11790, Egypt 2 Pharmaceutical Chemistry Department, Faculty of Pharmacy, King AbdulAziz University, Jeddah 21589, Kingdom of Saudi Arabia 3 Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo 11884, Egypt 4 Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11787, Egypt
* Author to whom correspondence should be addressed.
Received: 22 August 2012 / Revised: 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 (CC BY 3.0).

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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.

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