کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10593386 981806 2013 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists
چکیده انگلیسی
This Letter describes the discovery of GSK189254 and GSK239512 that were progressed as clinical candidates to explore the potential of H3 receptor antagonists as novel therapies for the treatment of Alzheimer's disease and other dementias. By carefully controlling the physicochemical properties of the benzazepine series and through the implementation of an aggressive and innovative screening strategy that employed high throughput in vivo assays to efficiently triage compounds, the medicinal chemistry effort was able to rapidly progress the benzazepine class of H3 antagonists through to the identification of clinical candidates with robust in vivo efficacy and excellent developability properties.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 24, 15 December 2013, Pages 6890-6896
نویسندگان
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