Synthesis and Analgesic Activity Evaluation of Some Agmatine Derivatives

Molecules

Hongxia He¹  Mengjia Liu¹  Zhibing Zheng²   Ying Liu²  Junhai Xiao²  Ruibin Su²  Chun Hu¹  Jin Li² 

[1] School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, 110016, P.R. China;Department of Medicinal Chemistry, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P.R. China

关键词: Agmatine derivatives;    synthesis;    analgesic activity;    blood-brain barrier;    opioid dependence;   

DOI  :  10.3390/11060393

来源: mdpi

【 摘 要 】

A series of N,N’-disubstituted-2-nitroethene-1,1-diamine and N,N’-disubstituted-N’’-cyanoguanidine derivatives were prepared and evaluated for in vivo analgesic activity. The blood brain barrier (BBB) VolSurf model was used to predict the BBB permeation profiles of our synthesized compounds. Some compounds show both remarkable analgesic activity and good BBB permeation profiles, and these compounds might be developed for treatment of opioid tolerance and dependence.

【 授权许可】

Unknown   
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