Morikawa A, Sone T, Asano T
Department of Medicinal Chemistry, Asahi Chemical Industry Co., Ltd., Miyazaki, Japan.
J Med Chem. 1989 Jan;32(1):42-6. doi: 10.1021/jm00121a009.
Two novel series of N-(2-guanidinoalkyl)-5-isoquinolinesulfonamides, 2 and 3, were prepared. Many of the compounds possessed vasodilatory activity when injected locally into the femoral artery of dogs. The most potent compound, 1-amidino-4-(5-isoquinolylsulfonyl)-1,4-perhydrodiazepine, 33, was comparable to diltiazem, which is used clinically as a vasodilator.
制备了两个新型的N-(2-胍基烷基)-5-异喹啉磺酰胺系列化合物，即2和3。许多化合物在局部注射到犬股动脉时具有血管舒张活性。最有效的化合物1-脒基-4-(5-异喹啉基磺酰基)-1,4-全氢二氮杂卓（33），与临床上用作血管舒张剂的地尔硫卓相当。
