کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373776 | 981906 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists](/preview/png/1373776.png)
چکیده انگلیسی
The discovery, synthesis, and preliminary structure–activity relationship (SAR) of a novel class of vasopressin V3 (V1b) receptor antagonists is described. Compound 1, identified by high throughput screening of a diverse, three million-member compound collection, prepared using ECLiPS™ technology, had good activity in a V3 binding assay (IC50 = 0.20 μM), but less than desirable physicochemical properties. Optimization of compound 1 yielded potent analogs 19 (IC50 = 0.31 μM) and 24 (IC50 = 0.12 μM) with improved drug-like characteristics.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 18, 15 September 2010, Pages 5394–5397
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 18, 15 September 2010, Pages 5394–5397
نویسندگان
Jeffrey J. Letourneau, Christopher M. Riviello, Hong Li, Andrew G. Cole, Koc-Kan Ho, Heather A. Zanetakos, Hema Desai, Jiuqiao Zhao, Douglas S. Auld, Susan E. Napier, Fiona J. Thomson, Katharine A. Goan, J. Richard Morphy, Michael H.J. Ohlmeyer,