کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1357750 | 981276 | 2015 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and synthesis of piperazine derivatives as a novel class of γ-secretase modulators that selectively lower Aβ42 production
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Novel piperazine derivatives as γ-secretase modulators (GSMs) were prepared and tested for their ability to selectively lower Aβ42 production. Lead compound 3, with selective Aβ42-lowering activity, was modified by replacing its imidazolylphenyl moiety with an oxazolylphenyl moiety. Optimization of the urea group significantly improved mouse microsomal stability, while retaining both activity and selectivity. These efforts led to the successful identification of an orally available and brain-penetrant GSM, 6j, which selectively reduced brain Aβ42 in mice.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 23, Issue 9, 1 May 2015, Pages 1923–1934
Journal: Bioorganic & Medicinal Chemistry - Volume 23, Issue 9, 1 May 2015, Pages 1923–1934
نویسندگان
Takafumi Takai, Tatsuki Koike, Eiji Honda, Yuichi Kajita, Minoru Nakamura, Sachie Morimoto, Yasutaka Hoashi, Makoto Kamata, Tomomichi Watanabe, Tomoko Igari, Jun Terauchi,