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Molecules 2015, 20(4), 5374-5391;

Anti-Inflammatory Screening and Molecular Modeling of Some Novel Coumarin Derivatives

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ain Helwan, Cairo 11790, Egypt
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 2 February 2015 / Revised: 1 March 2015 / Accepted: 3 March 2015 / Published: 26 March 2015
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [2188 KB, uploaded 26 March 2015]   |  


Coumarin and their derivatives have drawn much attention in the pharmacological and pharmaceutical fields due to their broad range and diverse biological activities. In the present work, starting from the 6-amino-7-hydroxy-4-methyl-2H-chromen-2-one, a series of 6-(substituted benzylamino)-7-hydroxy-4-methyl-2H-chromen-2-ones 111 was synthesized and assessed for their anti-inflammatory activity using the carrageenan-induced hind paw edema method. Compounds 2, 3, 4 and 9 showed significant (p < 0.001) reduction of rat paw edema volume after 1 h from the administration of the carrageenan compared to the reference drug, indomethacin. On the other hand, compounds 4 and 8 showed the highest anti-inflammatory activity, surpassing indomethacin after 3 h with 44.05% and 38.10% inhibition, respectively. Additionally, a molecular docking study was performed against the COX enzyme using the MOE 10.2010 software. View Full-Text
Keywords: 6-amino-8-hydroxycoumarin; anti-inflammatory; molecular docking 6-amino-8-hydroxycoumarin; anti-inflammatory; molecular docking

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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 (CC BY 4.0).

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El-Haggar, R.; Al-Wabli, R.I. Anti-Inflammatory Screening and Molecular Modeling of Some Novel Coumarin Derivatives. Molecules 2015, 20, 5374-5391.

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