کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1397461 1501168 2012 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
چکیده انگلیسی

In this work, we report a rational structure-based approach aimed at the discovery of new 2-aminoimidazoles as β-secretase inhibitors. Taking advantage of a microwave-assisted synthetic protocol, a small library of derivatives was obtained and biologically evaluated. Two compounds showed promising activities in both enzymatic and cellular assays. Moreover, one of them exhibited the capability to cross the blood–brain barrier as assessed by the parallel artificial membrane permeability assay.

Figure optionsDownload as PowerPoint slideHighlights
► BACE-1 inhibition as a validated AD modifying therapy.
► Rational structure-based design toward the discovery of new BACE-1 inhibitors.
► Application of a synthetic protocol amenable to parallel synthesis.
► Synthesis and biological evaluation of a small library of 2-aminoimidazoles.
► Compound 7 has emerged as a promising anti-BACE-1 hit compound.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 48, February 2012, Pages 206–213
نویسندگان
, , , , , , , , , , ,