کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10592821 981798 2014 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
(E)-Alkenes as replacements of amide bonds: Development of novel and potent acyclic CGRP receptor antagonists
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
(E)-Alkenes as replacements of amide bonds: Development of novel and potent acyclic CGRP receptor antagonists
چکیده انگلیسی
A new class of CGRP receptor antagonists was identified by replacing the central amide of a previously identified anilide lead structure with ethylene, ethane, or ethyne linkers. (E)-Alkenes as well as alkynes were found to preserve the proper bioactive conformation of the amides, necessary for efficient receptor binding. Further exploration resulted in several potent compounds against CGRP-R with low susceptibility to P-gp mediated efflux.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 1, 1 January 2014, Pages 258-261
نویسندگان
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