کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10592150 981777 2014 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and structure-activity relationship of dihydrobenzofuran derivatives as novel human GPR119 agonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and structure-activity relationship of dihydrobenzofuran derivatives as novel human GPR119 agonists
چکیده انگلیسی
Through appropriate medicinal chemistry design tactics and computer-assisted conformational modeling, the initial lead A was evolved into a series of dihydrobenzofuran derivatives 3 as potent GPR119 agonists. This Letter describes the optimization of general structure 3, including the substituent(s) on dihydrobenzofuran, the R1 attachment on right-hand piperidine nitrogen, and the left-hand piperidine/piperazine and its attachment R2. The efforts led to the identification of compounds 13c and 24 as potent human GPR119 modulators with favorable metabolic stability, ion channel activity, and PXR profiles.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 11, 1 June 2014, Pages 2539-2545
نویسندگان
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