Synthesis and anti-arrhythmic activity of some piperidine-based 1,3-thiazole, 1,3,4-thiadiazole, and 1,3-thiazolo[2,3-c]-1,2,4-triazole derivatives
作者:Hatem A. Abdel-Aziz、Bakr F. Abdel-Wahab、Marwa A. M. Sh. El-Sharief、Mohamed M. Abdulla
DOI:10.1007/s00706-008-0053-y
日期:2009.4
n-1-ylcarbonyl)acrylonitrile which was reacted with hydrazonoyl chlorides to yield the corresponding 1,3,4-thiadiazole derivatives. Some of the newly synthesized compounds had significant anti-arrhythmic activity. Graphical Abstract
摘要1- [4-(哌啶-1-基)亚苄基]硫代氨基脲与酰氯的反应得到1,3-噻唑衍生物。在室温下,在乙酸钠存在下,通过溴将后一种1,3-噻唑的两种化合物环化,得到1,3-噻唑并[2,3- c] -1,2,4-三唑衍生物。在三乙胺的存在下,在乙醇中回流下,使2-氰基-3-(4-哌啶-1-基苯基)丙-2-烯硫酰胺与no酰氯反应,得到1,3-噻唑。在环境温度下,在KOH存在下,在DMF中,用异硫氰酸苯酯处理3-氧代-3-(哌啶-1-基)丙烷腈,形成了3-苯胺基-3-巯基-2-(哌啶-使1-酰羰基)丙烯腈与酰氯反应,得到相应的1,3,4-噻二唑衍生物。一些新合成的化合物具有明显的抗心律不齐活性。 图形概要