کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370337 | 981816 | 2013 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
High throughput screening led to the identification of a novel series of quinolone α7 nicotinic acetylcholine receptor (nAChR) agonists. Optimization of an HTS hit (1) led to 4-phenyl-1-(quinuclidin-3-ylmethyl)quinolin-2(1H)-one, which was found to be potent and selective. Poor brain penetrance in this series was attributed to transporter-mediated efflux, which was in turn due to high pKa. A novel 4-fluoroquinuclidine significantly lowered the pKa of the quinuclidine moiety, reducing efflux as measured by a Caco-2 assay.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 6, 15 March 2013, Pages 1684–1688
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 6, 15 March 2013, Pages 1684–1688
نویسندگان
Ivar M. McDonald, Robert A. Mate, F. Christopher Zusi, Hong Huang, Debra J. Post-Munson, Meredith A. Ferrante, Lizbeth Gallagher, Robert L. Bertekap Jr., Ronald J. Knox, Barbara J. Robertson, David G. Harden, Daniel G. Morgan, Nicholas J. Lodge,