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发现新型 2-(4-(苄氧基)-5-(羟基)苯基)苯并噻唑衍生物作为治疗帕金森病的多功能 MAO-B 抑制剂。

Discovery of novel 2-(4-(benzyloxy)-5-(hydroxyl) phenyl) benzothiazole derivatives as multifunctional MAO-B inhibitors for the treatment of Parkinson's disease.

机构信息

School of Pharmacy, North Sichuan Medical College, Nanchong, China.

Sichuan Key Laboratory of Medical Imaging, School of Pharmacy and Nanchong Key Laboratory of MRI Contrast Agent, North Sichuan Medical College, Nanchong, China.

出版信息

J Enzyme Inhib Med Chem. 2023 Dec;38(1):2159957. doi: 10.1080/14756366.2022.2159957.

DOI:10.1080/14756366.2022.2159957
PMID:36728713
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9897792/
Abstract

To discover novel multifunctional agents for the treatment of Parkinson's disease, a series of 2-(4-(benzyloxy)-5-(hydroxyl) phenyl) benzothiazole derivatives was designed, synthesized and evaluated. The results revealed that representative compound possessed potent and selective MAO-B inhibitory activity (IC = 0.062 µM), and its inhibitory mode was competitive and reversible. Additionally, also displayed excellent anti-oxidative effect (ORAC = 2.27 Trolox equivalent), significant metal chelating ability and appropriate BBB permeability. Moreover, exhibited good neuroprotective effect and anti-neuroinflammtory ability. These results indicated that compound was a promising candidate for further development against PD.

摘要

为了发现治疗帕金森病的新型多功能药物，设计、合成并评价了一系列 2-(4-(苄氧基)-5-(羟基)苯基)苯并噻唑衍生物。结果表明，代表性化合物 对 MAO-B 具有很强的选择性抑制作用（IC = 0.062 µM），抑制模式为竞争性和可逆性。此外， 还表现出良好的抗氧化作用（ORAC = 2.27 Trolox 当量）、良好的金属螯合能力和适当的 BBB 渗透性。此外， 还表现出良好的神经保护作用和抗神经炎症作用。这些结果表明，化合物 是一种很有前途的候选药物，可进一步开发用于治疗 PD。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/452e5e6fd164/IENZ_A_2159957_F0007_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/33fcca24152d/IENZ_A_2159957_UF0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/ed538e092d8c/IENZ_A_2159957_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/90cfe9853080/IENZ_A_2159957_SCH0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/3b8650b3ead1/IENZ_A_2159957_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/72d9cf528b27/IENZ_A_2159957_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/3a25765eea8c/IENZ_A_2159957_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/c8dc1b8826ca/IENZ_A_2159957_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/51f03f6b6ea1/IENZ_A_2159957_F0006_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/452e5e6fd164/IENZ_A_2159957_F0007_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/33fcca24152d/IENZ_A_2159957_UF0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/ed538e092d8c/IENZ_A_2159957_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/90cfe9853080/IENZ_A_2159957_SCH0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/3b8650b3ead1/IENZ_A_2159957_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/72d9cf528b27/IENZ_A_2159957_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/3a25765eea8c/IENZ_A_2159957_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/c8dc1b8826ca/IENZ_A_2159957_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/51f03f6b6ea1/IENZ_A_2159957_F0006_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c4b/9897792/452e5e6fd164/IENZ_A_2159957_F0007_C.jpg

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2
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3
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