Synthesis and Biological Evaluation of Novel Bioisosteric Analogues of Dimebon (TM)

Alexandre Vasilevich Ivachtchenko, Eugene Borisovich Frolov,Oleg Dmitrievich Mitkin, Sergey Evgenevich Tkachenko,Alexandre Khvat

Letters in Drug Design & Discovery（2010）

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摘要

In the present paper, we describe the synthesis and biological evaluation for a series of novel 6,9-disubstituted 2-methyl-1,2,3,4,5,6-hexahydroazepino[4,3-b]indoles. These compounds represent unique bioisosteric analogues of Dimebon (TM) with promising biological activity against a panel of various targets including some GPCR family members.

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关键词

Dimebon (TM),Inhibitor,1,2,3,4,5,6-hexahydroazepino[4,3-b]indole,Alzheimer's disease,Parallel synthesis,GPCR,Analogues

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