Institute of Pharmaceutical Chemistry, ZAFES/LiFF/OSF, Goethe-University Frankfurt, Max-von-Laue-Str. 9, D-60438 Frankfurt/Main, Germany.
J Med Chem. 2013 Feb 28;56(4):1777-81. doi: 10.1021/jm301617j. Epub 2013 Feb 7.
Current research leads to the assumption that drugs affecting more than one target could result in a more efficient treatment of diseases and fewer safety concerns. Administration of drugs inhibiting only one branch of the arachidonic acid cascade is usually accompanied by side effects. We therefore designed and synthesized a library of hybrid molecules incorporating an imidazo[1,2-a]pyridine and an urea moiety as novel soluble epoxide hydrolase (sEH)/5-lipoxygenase (5-LO) dual inhibitors. Evaluation of the compounds was accomplished by in vitro testing using recombinant enzyme assays.
目前的研究假设，作用于多个靶点的药物可能会更有效地治疗疾病，且安全性顾虑也更少。通常，仅抑制花生四烯酸级联反应的一个分支的药物的给药会伴有副作用。因此，我们设计并合成了一个包含咪唑并[1,2-a]吡啶和脲部分的混合分子文库，作为新型可溶性环氧化物水解酶 (sEH)/5-脂氧合酶 (5-LO) 双重抑制剂。通过使用重组酶测定法进行体外测试来评估化合物。
