کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
7802480 | 1501159 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: Synthesis, biological assessment, and molecular modeling
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: Synthesis, biological assessment, and molecular modeling Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: Synthesis, biological assessment, and molecular modeling](/preview/png/7802480.png)
چکیده انگلیسی
⺠Pyridonepezils1-8 were designed and synthesized as dual AChEI, binding the CAS and PAS of the enzyme. ⺠The biological evaluation of molecules 1-8 showed that most of these compounds are potent AChEI. ⺠Compound 7, the most potent, is 703-fold more selective for hAChE than for hBuChE. ⺠The ability of compound 7 to interact with the PAS and CAS of AChE was confirmed by molecular modeling. ⺠Inhibitors 2-8 are permeable as determined in the PAMPA-BBB assay.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 57, November 2012, Pages 296-301
Journal: European Journal of Medicinal Chemistry - Volume 57, November 2012, Pages 296-301
نویسندگان
Abdelouahid Samadi, MartÃn Estrada, Concepción Pérez, MarÃa Isabel RodrÃguez-Franco, Isabel Iriepa, Ignacio Moraleda, Mourad Chioua, José Marco-Contelles,