一些与克罗卡林结构相关的N-芳基磺酰基-N-甲基-N'-(2,2-二甲基-2H-1-苯并吡喃-4-基)脲的合成与药理评价
Synthesis and pharmacological evaluation of some N-arylsulfonyl-N-methyl-N'-(2,2-dimethyl-2H-1-benzopyran-4-yl)ureas structurally related to cromakalim.
作者信息
Khelili Smail, Lebrun Philippe, de Tullio Pascal, Pirotte Bernard
机构信息
Laboratoire de Chimie Pharmaceutique, de Pharmacologie et d'Ecotoxicologie, Faculté des Sciences, Université de Jijel, B.P. 98 Ouled Aissa, 18000 Jijel, Algeria.
出版信息
Bioorg Med Chem. 2006 May 15;14(10):3530-4. doi: 10.1016/j.bmc.2006.01.009. Epub 2006 Feb 7.
Some N-arylsulfonyl-N-methyl-N'-(2,2-dimethyl-2H-1-benzopyran-4-yl)ureas were prepared and evaluated as putative potassium channel openers on the vascular and uterine smooth muscle tissue (myorelaxant effect), as well as on insulin-secreting pancreatic islets (inhibition of insulin release). The pharmacological results indicated that these compounds exhibited a marked biological activity on these three tissues.
制备了一些N-芳基磺酰基-N-甲基-N'-(2,2-二甲基-2H-1-苯并吡喃-4-基)脲，并作为假定的钾通道开放剂在血管和子宫平滑肌组织（肌松作用）以及胰岛素分泌胰腺胰岛（抑制胰岛素释放）上进行了评估。药理结果表明，这些化合物在这三种组织上均表现出显著的生物活性。
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