کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1370980 981834 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence
چکیده انگلیسی

We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced clearance, improved potency and is active in rat cystometry models of urinary incontinence after intravenous administration.

We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced clearance, improved potency and is active in rat cystometry models of urinary incontinence after intravenous administration.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 11, 1 June 2011, Pages 3354–3357
نویسندگان
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