Thiadiazolodiazepine analogues as a new class of neuromuscular blocking agents: Synthesis, biological evaluation and molecular modeling study

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• 作者：Hussein I. El-Subbagh^a ; ^{subbagh@yahoo.com} ; Adel S. El-Azab^b ; ^c ; Ghada S. Hassan^a ; Shahenda M. El-Messery^d ; Alaa A.-M. Abdel-Aziz^a ; ^b ; Kamal E.H. El-Taher^e
• 关键词：Synthesis ; Thiadiazolodiazepine analogues ; Neuromuscular blocking agents ; Molecular modeling study
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：15-23
• 全文大小：1128 K
• 卷排序：126

文摘

Synthesis of 6,7-dihydro-[1,3,4]thiadiazolo[3,2-a] [1,3]diazepines. Compounds GS-53 (30) and AAH1 (33) induced neuromuscular blockade. Compound 30 proved to be as twice as potent as 33 with rapid onset and shorter duration. Recognition with Thr120 and Thr124 at α7β2 nAChR receptor is essential for activity.