کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370802 | 981830 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Identification and optimisation of novel sulfonamide, selective vasopressin V1B receptor antagonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The synthesis and preliminary structure–activity relationships (SAR) of a novel class of vasopressin V1B receptor antagonists are described. Hit compound 5, identified via high throughput screening of the corporate collection, showed good activity in a V1B binding assay (Ki 63 nM) but did not possess the lead-like physicochemical properties typically required in a hit compound. A ‘deletion approach’ on the HTS hit 5 was performed, with the focus on improvement of physicochemical properties, yielding the selective V1B antagonist 9f (Ki 190 nM), with improved druglike characteristics.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 12, 15 June 2011, Pages 3603–3607
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 12, 15 June 2011, Pages 3603–3607
نویسندگان
James Baker, Matilda Bingham, Ruth Blackburn-Munro, Jiaqiang Cai, Mark Craighead, Robert Gilfillan, Kate Goan, David Jaap, Rachel Milne, J. Richard Morphy, Susan Napier, Jeremy Presland, Gayle Spinks, Fiona Thomson,