El-Haggar Radwan, Al-Wabli Reem I
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.
Molecules. 2015 Mar 26;20(4):5374-91. doi: 10.3390/molecules20045374.
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 1-11 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.
香豆素及其衍生物因其广泛多样的生物活性而在药理学和制药领域备受关注。在本研究中，以6-氨基-7-羟基-4-甲基-2H-色烯-2-酮为起始原料，合成了一系列6-（取代苄基氨基）-7-羟基-4-甲基-2H-色烯-2-酮1-11，并采用角叉菜胶诱导的后爪水肿法评估了它们的抗炎活性。与参比药物吲哚美辛相比，化合物2、3、4和9在给予角叉菜胶1小时后，大鼠爪水肿体积显著（p < 0.001）减小。另一方面，化合物4和8表现出最高的抗炎活性，在3小时后分别以44.05%和38.10%的抑制率超过了吲哚美辛。此外，使用MOE 10.2010软件针对COX酶进行了分子对接研究。
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