کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375116 | 981932 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The identification and hit-to-lead exploration of a novel, potent and selective series of histamine H4 receptor inverse agonists is described. The initial hit, 3A (IC50 19 nM) was identified by means of a ligand-based virtual screening approach. Subsequent medicinal chemistry exploration yielded 18I which possessed increased potency (R-enantiomer IC50 1 nM) as well as enhanced microsomal stability.
The hit-to-lead exploration of a series of novel, potent and selective series of histamine H4 receptor inverse agonists originating from a virtual screening approach is described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 8, 15 April 2010, Pages 2516–2519
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 8, 15 April 2010, Pages 2516–2519
نویسندگان
Sue Cramp, Hazel J. Dyke, Christopher Higgs, David E. Clark, Matthew Gill, Pascal Savy, Neil Jennings, Steve Price, Peter M. Lockey, Dennis Norman, Soraya Porres, Francis Wilson, Alison Jones, Nigel Ramsden, Raffaella Mangano, Dan Leggate,