کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1369722 981787 2016 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design and synthesis of aminothiazole modulators of the gamma-secretase enzyme
ترجمه فارسی عنوان
طراحی و سنتز تعدیل کننده های آمینوتیازول آنزیم گاما اسید
کلمات کلیدی
بیماری آلزایمر، مدولاتور γ-مخزن، آمینوتیازول
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

The design and construction of a series of novel aminothiazole-derived γ-secretase modulators is described. The incorporation of heterocyclic replacements of the terminal phenyl D-ring of lead compound 1 was conducted in order to align potency with favorable drug-like properties. γ-Secretase modulator 28 displayed good activity for in vitro inhibition of Aβ42, as well as substantial improvement in ADME and physicochemical properties, including aqueous solubility. Pharmacokinetic evaluation of compound 28 in mice revealed good brain penetration, as well as good clearance, half-life, and volume of distribution which collectively support the continued development of this class of compounds.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 16, 15 August 2016, Pages 3928–3937
نویسندگان
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