کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1370232 981814 2011 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Carbazole-containing arylcarboxamides as BACE1 inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Carbazole-containing arylcarboxamides as BACE1 inhibitors
چکیده انگلیسی

β-Secretase (BACE1) is widely recognized as a prime drug target for the treatment of Alzheimer’s disease (AD). In this Letter, we report the synthesis and the BACE1 inhibitory activity of novel, variously substituted N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-arylcarboxamides. The best results have been obtained with the introduction of a 4-OMe substituent (IC50 = 3.8 μM) or a 3,4-dichloro substituent (IC50 = 2.5 μM) in the amidic aromatic ring. The blood–brain barrier penetration predictions resulted to be promising for this type of compounds. To better understand the structure–activity relationships (SAR) of the new derivatives, a docking study procedure has been applied exploiting different conformational and ionic states of BACE1.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 22, 15 November 2011, Pages 6657–6661
نویسندگان
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