Novel Arylalkenylpropargylamines as Neuroprotective, Potent, and Selective Monoamine Oxidase B Inhibitors for the Treatment of Parkinson’s Disease
作者:Paul B. Huleatt、Mui Ling Khoo、Yi Yuan Chua、Tiong Wei Tan、Rou Shen Liew、Balázs Balogh、Ruth Deme、Flóra Gölöncsér、Kalman Magyar、David P. Sheela、Han Kiat Ho、Beáta Sperlágh、Péter Mátyus、Christina L. L. Chai
DOI:10.1021/jm501722s
日期:2015.2.12
To develop novel neuroprotective agents, a library of novel arylalkenylpropargylamines was synthesized and tested for inhibitory activities against monoamineoxidases. From this, a number of highly potent and selectivemonoamineoxidaseB inhibitors were identified. Selected compounds were also tested for neuroprotection in in vitro studies with PC-12 cells treated with 6-OHDA and rotenone, respectively
Organozirconium-Mediated Solution- and Solid-Phase Synthesis of 3-Benzyl Pyrrolidines and Other Potentially Neuroactive Amines
作者:Richard Whitby、Rupert Hunter、Donald Macfarlane
DOI:10.1055/s-2006-951553
日期:——
An efficient route to 3-benzylpyrrolidines using a zirconium-mediated cyclisation both in solution and on a solid support is reported. 3-Benzylidine-pyrrolidines, 3-aryl-pyrrolidines and 4-arylpiperidines were also synthesised.