89539-51-5Relevant articles and documents
N-Propargylamine-hydroxypyridinone hybrids as multitarget agents for the treatment of Alzheimer's disease
Guo, Jianan,Zhang, Yujia,Zhang, Changjun,Yao, Chuansheng,Zhang, Jingqi,Jiang, Xiaoying,Zhong, Zhichao,Ge, Jiamin,Zhou, Tao,Bai, Renren,Xie, Yuanyuan
, (2021/06/07)
AD is a progressive brain disorder. Because of the lack of remarkable single-target drugs against neurodegenerative disorders, the multitarget-directed ligand strategy has received attention as a promising therapeutic approach. Herein, we rationally designed twenty-nine hybrids of N-propargylamine-hydroxypyridinone. The designed hybrids possessed excellent iron-chelating activity (pFe3+ = 17.09–22.02) and potent monoamine oxidase B inhibitory effects. Various biological evaluations of the optimal compound 6b were performed step by step, including inhibition screening of monoamine oxidase (hMAO-B IC50 = 0.083 ± 0.001 μM, hMAO-A IC50 = 6.11 ± 0.08 μM; SI = 73.5), prediction of blood–brain barrier permeability and mouse behavioral research. All of these favorable results proved that the N-propargylamine-hydroxypyridinone scaffold is a promising structure for the discovery of multitargeted ligands for AD therapy.
Pyridone hexa-alkyne amine modified derivative and preparation method and application thereof
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Paragraph 0085; 0088, (2021/03/30)
The invention relates to a pyridone hexa-alkyne amine modified derivative as shown in a formula (I) and a pharmaceutically acceptable salt thereof, a preparation method thereof, application of the pyridone hexa-alkyne amine modified derivative or the pharmaceutically acceptable salt thereof to preparation of drugs for preventing or treating related diseases, especially Alzheimer's disease and Parkinson's disease, by inhibiting monoamine oxidase, chelating metal iron ions, resisting Abeta and resisting oxidation. According to the invention, a series of novel single-molecule multi-target anti-ADactive compounds are synthesized, and pyridone derivatives with iron ion chelating activity and propynylamine with MAOB inhibitory activity are creatively and organically combined together, so that the compounds have remarkable advantages on Alzheimer's disease with complex pathogenesis; and the combined molecules are far superior to CP20 (deferiprone) in the aspect of iron ion chelating activity.
ALA-HPO hybrid derivative with iron chelating property and PDT activity, preparation method and application thereof
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Paragraph 0074; 0078, (2020/12/30)
The invention provides an ALA-HPO hybrid derivative shown as a formula (I) or a formula (II), and a preparation method thereof, and application of the ALA-HPO hybrid derivative in preparation of photodynamic therapy drugs. The formula (I) and the formula (II) are defined in the specification.