Bruno Olga, Brullo Chiara, Bondavalli Francesco, Ranise Angelo, Schenone Silvia, Falzarano Maria Sofia, Varani Katia, Spisani Susanna
Dipartimento di Scienze Farmaceutiche, Università di Genova, Genova, Italy.
Bioorg Med Chem Lett. 2007 Jul 1;17(13):3696-701. doi: 10.1016/j.bmcl.2007.04.036. Epub 2007 Apr 19.
It is well known that both acute and chronic autoimmune inflammatory disorders arise following a breakdown in control of neutrophil activation and recruitment. In the search for new anti-inflammatory agents, we synthesized some new 2-phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives and tested them in vitro in order to evaluate their ability to interfere with human neutrophil functions. All tested compounds showed strong inhibition of fMLP-OMe-induced chemotaxis, although they appeared unable to block degranulation and the fMLP-OMe-induced respiratory burst, and were inactive in binding experiments.
众所周知，急性和慢性自身免疫性炎症性疾病是在中性粒细胞激活和募集控制失效后出现的。在寻找新的抗炎剂的过程中，我们合成了一些新的2-苯基-2,3-二氢-1H-咪唑并[1,2-b]吡唑衍生物，并在体外对它们进行了测试，以评估它们干扰人类中性粒细胞功能的能力。所有测试的化合物都表现出对fMLP-OMe诱导的趋化作用有强烈抑制作用，尽管它们似乎无法阻断脱颗粒和fMLP-OMe诱导的呼吸爆发，并且在结合实验中无活性。
