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Design, Synthesis and Evaluation of 3-Substituted Coumarin Derivatives as Anti-inflammatory Agents.
Chemical & Pharmaceutical Bulletin ( IF 1.7 ) Pub Date : 2020-03-13 , DOI: 10.1248/cpb.c19-01085
Tao Wang 1, 2 , Tao Peng 2 , Xiaoxue Wen 2 , Gang Wang 2 , Shuchen Liu 2 , Yunbo Sun 2 , Shouguo Zhang 2 , Lin Wang 1, 2
Affiliation  

Coumarin moiety has garnered momentous attention especially in the design of compounds with significant biological activities. In this work, a series of 3-substituted coumarin derivatives 6a-6l were synthesized and fully characterized. Most of the compounds could obviously inhibit the activity of cyclooxygenase-1 (COX-1) at the concentration of 10 µM. Besides, 6h and 6l exhibited highest inhibitory effects against COX-2 with inhibition rates of 33.48 and 35.71%, respectively. Detailed structure-activity relationships (SARs) were also discussed. In vivo studies, 6b, 6i and 6l could remarkably repress the xylene-induced ear swelling in mice at the dose of 20 mg/kg. Especially, 6l seemed to be the most effective compound at the dose of 10 mg/kg, displaying favorable anti-inflammatory activity comparable to indomethacin. All of these findings suggested that 6l might be utilized as a candidate for the treatment of inflammatory diseases.

中文翻译:

设计,合成和评估3-取代香豆素衍生物作为抗炎药。

香豆素部分已经引起了广泛的关注,特别是在具有显着生物学活性的化合物的设计中。在这项工作中,合成并充分表征了一系列3-取代的香豆素衍生物6a-6l。在10 µM的浓度下,大多数化合物都能明显抑制环氧合酶1(COX-1)的活性。此外,6h和6l对COX-2的抑制作用最高,抑制率分别为33.48%和35.71%。还讨论了详细的结构-活性关系(SAR)。在体内研究中,6b,6i和6l可以以20 mg / kg的剂量显着抑制小鼠体内由二甲苯引起的耳肿。特别地,在10mg / kg的剂量下6l似乎是最有效的化合物,表现出与消炎痛相当的有利的抗炎活性。
更新日期:2020-03-13
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