کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10593122 981804 2012 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and evaluation of 4-alkoxy-[1′-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4′-piperidine)] analogues as histamine-3 receptor antagonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and evaluation of 4-alkoxy-[1′-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4′-piperidine)] analogues as histamine-3 receptor antagonists
چکیده انگلیسی
A novel class of 4-alkoxy-[1′-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4′-piperidine)] analogues were designed and synthesized as H3R antagonists. Structure-activity relationship identified sulfone 27 with excellent H3R affinities in both humans and rats, and acceptable pharmacokinetic properties. Further, compound 28 achieved single digit nanomolar H3R affinities in both species with minimum hERG activity.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 1, 1 January 2012, Pages 186-189
نویسندگان
, , , , , ,