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Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors.

Abstract：

:A series of 9-aminoalkanamido-1-azabenzanthrones derviatives (3a-i Ar-NHCO(CH(2))(n)NR(1)R(2)) and their quaternary methiodide salts (4a-g Ar-NHCO(CH(2))(n)N(+)(CH(3))R(1)R(2)I(-)) were designed and synthesized as acetylcholinesterase (AChE) or butyrylcholinesterase (BuChE) inhibitors. The synthetic compounds exhibited high AChE inhibitory activity with IC(50) values in the nanomolar range and high selectivity for AChE over BuChE (45- to 1980-fold). The structure-activity relationships (SARs) were discussed.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Tang H,Ning FX,Wei YB,Huang SL,Huang ZS,Chan AS,Gu LQ

doi

10.1016/j.bmcl.2007.04.015

subject

Has Abstract

pub_date

2007-07-01 00:00:00

pages

3765-8

issue

13

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00431-3

journal_volume

17

pub_type

杂志文章

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