2-phenyl-benzo nitrogen-containing heterocyclic compound as well as preparation method and application thereof

By developing 2-phenyl-benzo nitrogen-containing heterocyclic compounds, especially compound 34, the problem of difficult to provide effective small molecule 17β-HSD10 inhibitors in the prior art is solved, and effective inhibition of 17β-HSD10 and potential therapeutic effects of Alzheimer's disease are achieved.

CN119707829APending Publication Date: 2025-03-28HEFEI UNIV
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Patent Information

Application Number
CN202411634998.0
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-11-15
Publication Date
2025-03-28

AI Technical Summary

Technical Problem

The prior art is difficult to provide effective and selective small molecule 17β-HSD10 inhibitors for the treatment of Alzheimer's disease.

Method used

A 2-phenyl-benzo nitrogen-containing heterocyclic compound was developed, and a compound 34 with inhibiting 17β-HSD10 activity was prepared through specific synthesis routes, such as the cyclic reaction of 3,5-dimethyl-1,2-phenyldiamine and benzaldehyde derivatives, nitro reduction, condensation reaction and other steps.

Benefits of technology

Compound 34 showed similar inhibitory activity to the positive control 17β-HSD10-IN-1 and was low toxicity with potential for the treatment of Alzheimer's disease.

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Abstract

The invention discloses a 2-phenyl-benzo nitrogen-containing heterocyclic compound as well as a preparation method and application thereof, and relates to the technical field of medicinal chemistry, the structural formula of the 2-phenyl-benzo nitrogen-containing heterocyclic compound is as shown in a formula I and a formula II: # imgabs0 #. The 2-phenyl-benzo nitrogen-containing heterocyclic compound disclosed by the invention shows certain inhibitory activity on 17 beta-HSD10; wherein the compound 34 has the best inhibitory activity, has a treatment effect on scopolamine-induced mouse cognitive impairment, is relatively low in toxicity, and is expected to be applied to preparation of medicines for treating AD (Alzheimer's disease).
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