期刊
MOLECULES
卷 22, 期 8, 页码 -出版社
MDPI
DOI: 10.3390/molecules22081265
关键词
acetylcholinesterase; Alzheimer's disease; butyrylcholinesterase; tacrine; 7-MEOTA; huprine Y; 2-methoxyhuprine
资金
- Ministry of Health of the Czech Republic [15-30954A]
- COST Action [CA15135]
- MEYS under the NPU I program [LO1611]
- Ministry of Defence Long Term Development Plan
- Ministry of Education, Youth and Sports of the Czech Republic under the Projects CESNET [LM2015042]
- CERIT-Scientific Cloud [LM2015085]
Tacrine (THA), the first clinically effective acetylcholinesterase (AChE) inhibitor and the first approved drug for the treatment of Alzheimer's disease (AD), was withdrawn from the market due to its side effects, particularly its hepatotoxicity. Nowadays, THA serves as a valuable scaffold for the design of novel agents potentially applicable for AD treatment. One such compound, namely 7-methoxytacrine (7-MEOTA), exhibits an intriguing profile, having suppressed hepatotoxicity and concomitantly retaining AChE inhibition properties. Another interesting class of AChE inhibitors represents Huprines, designed by merging two fragments of the known AChE inhibitors-THA and (-)-huperzine A. Several members of this compound family are more potent human AChE inhibitors than the parent compounds. The most promising are so-called huprines X and Y. Here, we report the design, synthesis, biological evaluation, and in silico studies of 2-methoxyhuprine that amalgamates structural features of 7-MEOTA and huprine Y in one molecule.
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