کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1377548 981981 2007 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine
چکیده انگلیسی

SAR studies on amides, ureas, and vinylogous amides derived from pyrrolidine led to the discovery of several potent hNK1 antagonists. One particular vinylogous amide (45b) had excellent potency, selectivity, pharmacokinetic profile, and functional activity in vivo. An in vivo rhesus macaque brain receptor occupancy PET study for compound 45b revealed an estimated Occ90 ∼ 300 ng/ml.

SAR studies on amides, ureas, and vinylogous amides derived from pyrrolidine led to the discovery of several potent hNK1 antagonists. One vinylogous amide (45b) had excellent potency, selectivity, pharmacokinetic profile, and functional activity in vivo. An in vivo rhesus macaque brain receptor occupancy PET study for compound 45b revealed an estimated Occ90 ∼ 300 ng/ml.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 18, 15 September 2007, Pages 5191–5198
نویسندگان
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