کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10595537 981873 2013 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 receptor antagonist
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 receptor antagonist
چکیده انگلیسی
A convergent synthesis route for the heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 antagonist 2 was developed and the structure activity relationship of these modifications on NPY1 binding is reported. Two heterocyclic analogs 9 and 10 showed comparable Y1 binding potency to 2, but with improved aqueous solubility. Compound 9 demonstrated reduced spontaneous nocturnal food intake in a rat model when dosed ip. Compound 9 was also shown to be orally bioavailable and brain penetrable.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 13, 1 July 2013, Pages 3814-3817
نویسندگان
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