【摘 要】
：
Acetylcholinesterase inhibitors are the most frequently prescribed anti-Alzheimers drugs.A series of 6-acetyl-5H-thiazolo[3,2-a]pyrimidine derivatives as th
【机 构】
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Shenyang Pharmaceutical University,Shenyang 110016
【出 处】
：
第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
Acetylcholinesterase inhibitors are the most frequently prescribed anti-Alzheimers drugs.A series of 6-acetyl-5H-thiazolo[3,2-a]pyrimidine derivatives as the novel acetylcholinesterase inhibitors were designed based on virtual screening methods.The target compounds were synthesized with Biginelli reaction and Hantzsch-type condensation of dihydropyrimidines with substituted phenacyl chlorides,and were characterized with elemental analysis,IR,MS,NMR.The biological evaluation against human acetylcholinesterase in vitro showed most target compounds exhibited varying inhibition at 10 μM using the Ellman method.The preliminary structure-activity relationships were the 2-hydroxyethoxy group at the phenyl ring at C4 position of the parent nucleus played significant roles in the AChE inhibitory activity of the target compounds.
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