کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1370031 981802 2016 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, and analysis of antagonists of GPR55: Piperidine-substituted 1,3,4-oxadiazol-2-ones
ترجمه فارسی عنوان
طراحی، سنتز و تجزیه و تحلیل آنتاگونیست GPR55: Piperidine-substituted 1،3،4-oxadiazol-2-ones
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

A series of 1,3,4-oxadiazol-2-ones was synthesized and tested for activity as antagonists at GPR55 in cellular beta-arrestin redistribution assays. The synthesis was designed to be modular in nature so that a sufficient number of analogues could be rapidly accessed to explore initial structure–activity relationships. The design of analogues was guided by the docking of potential compounds into a model of the inactive form of GPR55. The results of the assays were used to learn more about the binding pocket of GPR55. With this oxadiazolone scaffold, it was determined that modification of the aryl group adjacent to the oxadiazolone ring was often detrimental and that the distal cyclopropane was beneficial for activity. These results will guide further exploration of this receptor.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 7, 1 April 2016, Pages 1827–1830
نویسندگان
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