Journal of the Serbian Chemical Society 2015 Volume 80, Issue 2, Pages: 127-136
https://doi.org/10.2298/JSC140319092Z
Full text (
252 KB)
Cited by
Novel hybrids of oxoisoaporphine-tryptamine as acetylcholinesterase-induced β-amyloid aggregation inhibitors with improved antioxidant properties
Zhao Hai-Tao (School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University, Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guilin, P.R. China)
Zhong Shu-Ming (School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University, Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guilin, P.R. China)
Qin Jiang-Ke (School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University, Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guilin, P.R. China)
Tang Huang (School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University, Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guilin, P.R. China)
A series of dual binding site acetylcholinesterase (AChE) inhibitors have
been designed, synthesized, and tested for their antioxidant ability and
inhibitory potency on AChE and AChE-induced b-amyloid (Ab) aggregation. The
new hybrids consist of a unit of 1-azabenzanthrone and a tryptamine or its
derivative, connected through a a,w - alkyldiamide bridge. These hybrids
exhibit moderate AChE inhibitory activity with IC50 values in the micromolar
range and significant in vitro inhibitory activity toward the AChE-induced Ab
aggregation. Moreover, six out of the nine hybrids of this series exhibit a
higher oxygen radical absorbance capacity than trolox, which makes them
promising anti-Alzheimer drug candidates.
Keywords: Alzheimer’s disease, acetylcholinesterase inhibitor, Ab antiag-gregating activity, oxoisoaporphine-tryptamine