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Fudan University

Zheng Xia

Hao Wang

Xinghai Wang

Hongzhuan Chen

Qiong Xie

Meiyan Lu

Zhuibai Qiu

The present invention belongs to pharmaceutical field. It relates to a novel family of bivalent (&#x2212;)-meptazinol compounds and/or their salts, as well as the preparation and utilization of the compounds in the treatment of neurodegenerative disorders and dementias such as Alzheimer's Disease (AD). In the present invention, bivalent (&#x2212;)-meptazinol compounds were synthesized, from the starting material (&#x2212;)-meptazinol, successively by N-demethylation forming (&#x2212;)-nor-meptazinol and then by acylation with &#x3b1;,&#x3c9;-alkanediacyl dihalides or alkylation with &#x3b1;,&#x3c9;-dihaloalkanes. Results from in vitro cholinesterase inhibiting test and AChE-induced A&#x3b2; aggregation test demonstrated that the bivalent (&#x2212;)-meptazinol compounds and/or their salts were novel bivalent inhibitors of both AChE and A&#x3b2; aggregation. The most potent compound inhibited both AChE and BChE at nM level, which was 10000 and 1500 times more potent than (&#x2212;)-MEP hydrochloride, respectively. It inhibited AChE-induced A&#x3b2; aggregation by a factor of 2 compared with propidium.

Bivalent (&#x2212;)-meptazinol compounds and/or their salts, and their preparation and futilization

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Shanghai, China

Zheng Xia