Harrak Y, Rosell G, Daidone G, Plescia S, Schillaci D, Pujol M D
Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, Universitat de Barcelona, Av. Diagonal 643, E-08028 Barcelona, Spain.
Bioorg Med Chem. 2007 Jul 15;15(14):4876-90. doi: 10.1016/j.bmc.2007.04.050. Epub 2007 May 3.
A series of substituted derivatives containing the 1,4-benzodioxine or pyrrole nucleus are described. All the newly synthesized compounds were examined for their in vitro and in vivo anti-inflammatory activity. Several derivatives, including (S)-2, 14 and 17, showed more anti-inflammatory activity in vivo in these assays (rat paw oedema induced by carrageenan) than the known classical anti-inflammatory agent ibuprofen, whereas other compounds like 1 were equipotent to ibuprofen. Compound 17 was the most outstanding derivative because of its remarkable in vivo anti-inflammatory activity. In this paper, we examine and discuss the structure-activity relationships and anti-inflammatory activities of these compounds.
描述了一系列含有1,4-苯并二恶英或吡咯核的取代衍生物。对所有新合成的化合物进行了体外和体内抗炎活性检测。在这些实验（角叉菜胶诱导的大鼠足肿胀）中，包括(S)-2、14和17在内的几种衍生物在体内显示出比已知的经典抗炎药布洛芬更强的抗炎活性，而其他化合物如1与布洛芬的活性相当。化合物17因其显著的体内抗炎活性而成为最突出的衍生物。本文研究并讨论了这些化合物的构效关系和抗炎活性。
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