دورية أكاديمية
Multitarget drugs as potential therapeutic agents for alzheimer’s disease. A new family of 5-substituted indazole derivatives as cholinergic and BACE1 inhibitors
| العنوان: | Multitarget drugs as potential therapeutic agents for alzheimer’s disease. A new family of 5-substituted indazole derivatives as cholinergic and BACE1 inhibitors |
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| المؤلفون: | Pedro González-Naranjo, Concepción Pérez, Marina González-Sánchez, Adrián Gironda-Martínez, Eugenia Ulzurrun, Fernando Bartolomé, Marcos Rubio-Fernández, Angeles Martin-Requero, Nuria E. Campillo, Juan A. Páez |
| المصدر: | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 2348-2356 (2022) |
| بيانات النشر: | Taylor & Francis Group, 2022. |
| سنة النشر: | 2022 |
| المجموعة: | LCC:Therapeutics. Pharmacology |
| مصطلحات موضوعية: | Alzheimer’s disease, BACE1 inhibitor, BuChE inhibitor, indazole, multitarget drug, Therapeutics. Pharmacology, RM1-950 |
| الوصف: | Multitarget drugs are a promising therapeutic approach against Alzheimer’s disease. In this work, a new family of 5-substituted indazole derivatives with a multitarget profile including cholinesterase and BACE1 inhibition is described. Thus, the synthesis and evaluation of a new class of 5-substituted indazoles has been performed. Pharmacological evaluation includes in vitro inhibitory assays on AChE/BuChE and BACE1 enzymes. Also, the corresponding competition studies on BuChE were carried out. Additionally, antioxidant properties have been calculated from ORAC assays. Furthermore, studies of anti-inflammatory properties on Raw 264.7 cells and neuroprotective effects in human neuroblastoma SH-SY5Y cells have been performed. The results of pharmacological tests have shown that some of these 5-substituted indazole derivatives 1–4 and 6 behave as AChE/BuChE and BACE1 inhibitors, simultaneously. In addition, some indazole derivatives showed anti-inflammatory (3, 6) and neuroprotective (1–4 and 6) effects against Aβ-induced cell death in human neuroblastoma SH-SY5Y cells with antioxidant properties. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 14756366 1475-6374 1475-6366 |
| Relation: | https://doaj.org/toc/1475-6366; https://doaj.org/toc/1475-6374 |
| DOI: | 10.1080/14756366.2022.2117315 |
| URL الوصول: | https://doaj.org/article/4413ef31a44a48d79464776ae07d0209 |
| رقم الأكسشن: | edsdoj.4413ef31a44a48d79464776ae07d0209 |
| قاعدة البيانات: | Directory of Open Access Journals |
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Full Text Finder | تدمد: | 14756366 14756374 |
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| DOI: | 10.1080/14756366.2022.2117315 |