5-Isoquinolinesulfonamide derivatives. 1. Synthesis and vasodilatory activity of N-(2-guanidinoethyl)-5-isoquinolinesulfonamide derivatives.
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.
Morikawa
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Department of Medicinal Chemistry, Asahi Chemical Industry Co., Ltd., Miyazaki, Japan.
Sone
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Asano
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D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis; D004285:Dogs; D005260:Female; D005263:Femoral Artery / Q000187:drug effects; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D014665:Vasodilator Agents / Q000138:chemical synthesis*
D002121:Calcium Channel Blockers; D007546:Isoquinolines; D013449:Sulfonamides; D014665:Vasodilator Agents; C043204:N-(2-guanidinoethyl)-5-isoquinolinesulfonamide