Benzamide-oxadiazole skeleton compound as well as preparation method and application thereof

By synthesizing compounds with a benzamide-oxadiazole structure, selective inhibition of BChE and activation of Nrf2 were achieved, solving the problem that existing AD treatments cannot effectively intervene in the pathological mechanism, significantly improving cognitive function and providing neuroprotection.

CN121537360APending Publication Date: 2026-02-17CHINA PHARM UNIV
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Patent Information

Application Number
CN202511759656.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-11-27
Publication Date
2026-02-17

AI Technical Summary

Technical Problem

Existing Alzheimer's disease treatments cannot effectively address the underlying pathological mechanisms of the disease and pose safety risks, thus failing to meet clinical needs.

Method used

The goal is to develop compounds with a benzamide-oxadiazole structure that achieve dual synergistic pharmacological effects by simultaneously inhibiting BChE and activating the Nrf2 signaling pathway. The preparation method involves synthesizing intermediates and target compounds under specific conditions.

Benefits of technology

The compound showed good and highly selective inhibitory ability against BChE, effectively activated antioxidant pathways, significantly improved cognitive dysfunction in AD model animals, had neuroprotective effects, and delayed disease progression.

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Abstract

The invention discloses a compound with a benzamide-oxadiazole skeleton as well as a preparation method and application thereof. The structure of the compound is shown in the specification. According to the present invention, butyrylcholine esterase inhibition activity, Nrf2 activation activity, in vitro pharmacodynamic experiment and Morris water maze experiment are adopted as carriers to evaluate the treatment of Alzheimer's disease (especially moderate and severe Alzheimer's disease) by using the compound represented by the general formula I, and the results show that the compound has good in vitro and in vivo activity and extremely high selectivity; the compound can be used as a candidate lead compound for further development of an anti-Alzheimer's disease effect by selectively inhibiting butyrylcholine esterase and activating Nrf2.
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