کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10586805 | 981396 | 2014 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The effect of pKa on pyrimidine/pyridine-derived histamine H4 ligands
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
During the course of our efforts toward the discovery of human histamine H4 antagonists from a series of 2-aminiopyrimidines, it was noted that a 6-trifluoromethyl group dramatically reduced affinity of the series toward the histamine H4 receptor. This observation was further investigated by synthesizing a series of ligands that varied in pKa of the pyrimidine derived H4 ligands by over five orders of magnitude and the effect on histamine H4 affinity. This trend was then extended to the discovery of C-linked piperidinyl-2-amino pyridines as histamine H4 receptor antagonists.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 23, 1 December 2014, Pages 5489-5492
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 23, 1 December 2014, Pages 5489-5492
نویسندگان
Brad M. Savall, Steven P. Meduna, Jennifer Venable, Jianmei Wei, Russell C. Smith, Michael D. Hack, Robin L. Thurmond, Patricia McGovern, James P. Edwards,