کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10592477 | 981794 | 2012 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Triazoloamides as potent γ-secretase modulators with reduced hERG liability
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Triazoloamides as potent γ-secretase modulators with reduced hERG liability Triazoloamides as potent γ-secretase modulators with reduced hERG liability](/preview/png/10592477.png)
چکیده انگلیسی
Synthesis and SAR studies of novel aryl triazoles as gamma secretase modulators (GSMs) are presented in this communication. Starting from our aryl triazole leads, optimization studies were continued and the series progressed towards novel amides and lactams. Triazole 57 was identified as the most potent analog in this series, displaying single-digit nanomolar Aβ42 IC50 in cell-based assays and reduced affinity for the hERG channel.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 9, 1 May 2012, Pages 3140-3146
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 9, 1 May 2012, Pages 3140-3146
نویسندگان
Christian Fischer, Susan L. Zultanski, Hua Zhou, Joey L. Methot, Sanjiv Shah, Hugh Nuthall, Bethany L. Hughes, Nadja Smotrov, Armetta Hill, Alexander A. Szewczak, Christopher M. Moxham, Nathan Bays, Richard E. Middleton, Benito Munoz, Mark S. Shearman,