106840-17-9Relevant articles and documents
Compound and its as L-type calcium channel blocker or/and application of acetylcholine esterase inhibitors
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Paragraph 0317-0318, (2016/10/07)
Disclosed in this invention are compounds and the uses as L-type calcium channel blocker and/or acetylcholinesterase inhibitor thereof. The uses of said compounds in the manufactures of a medicament for the treatment of cardiovascular diseases, apoplexy or senile dementia are also disclosed in the present invention.
A conformational restriction approach to the development of dual inhibitors of acetylcholinesterase and serotonin transporter as potential agents for Alzheimer's disease
Toda, Narihiro,Tago, Keiko,Marumoto, Shinji,Takami, Kazuko,Ori, Mayuko,Yamada, Naho,Koyama, Kazuo,Naruto, Shunji,Abe, Kazumi,Yamazaki, Reina,Hara, Takao,Aoyagi, Atsushi,Abe, Yasuyuki,Kaneko, Tsugio,Kogen, Hiroshi
, p. 4389 - 4415 (2007/10/03)
Alzheimer's disease (AD) has been treated with acetylcholinesterase (AChE) inhibitors such as donepezil. However, the clinical usefulness of AChE inhibitors is limited mainly due to their adverse peripheral effects. Depression seen in AD patients has been treated with serotonin transporter (SERT) inhibitors. We considered that combining SERT and AChE inhibition could improve the clinical usefulness of AChE inhibitors. In a previous paper, we found a potential dual inhibitor, 1, of AChE (IC50=101 nM) and SERT (IC50=42 nM), but its AChE inhibition activity was less than donepezil (IC50=10 nM). Here, we report the conformationally restricted (R)-18a considerably enhanced inhibitory activity against AChE (IC50=14 nM) and SERT (IC50=6 nM).