کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10587896 981444 2013 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design and synthesis of imidazole and triazole derivatives as Lp-PLA2 inhibitors and the unexpected discovery of highly potent quaternary ammonium salts
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design and synthesis of imidazole and triazole derivatives as Lp-PLA2 inhibitors and the unexpected discovery of highly potent quaternary ammonium salts
چکیده انگلیسی
New Lp-PLA2 inhibitors were synthesized by the bioisosteric replacement of the amide group of Darapladib with an imidazole or a triazole. Unfortunately, the inhibitory activities of these derivatives were lower than that of Darapladib. But interestingly, a series of quaternary ammonium salts that were isolated as by-products during this synthetic work were found with high potency. Of these by-products, compound 22c showed a similar profile to Darapladib both in vitro and in vivo.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 5, 1 March 2013, Pages 1187-1192
نویسندگان
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