کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374571 | 981921 | 2010 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
PDE4 inhibitors are a validated approach as anti-inflammatory agents but are limited by systemic side effects including emesis. We report a soft-drug strategy incorporating a carboxylic ester group into boron-containing PDE4 inhibitors leading to the discovery of a series of benzoxaborole compounds with good potency (for example IC50 = 47 nM of compound 2) and low emetic activity. These compounds are intended for dermatological use further limiting possible systemic side effects.
A carboxylic ester group is incorporated into boron-containing PDE4 inhibitors leading to the discovery of benzoxaborole carboxylic ester compounds with good potency against PDE4 and low emetic activity.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 7, 1 April 2010, Pages 2270–2274
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 7, 1 April 2010, Pages 2270–2274
نویسندگان
Yong-Kang Zhang, Jacob J. Plattner, Tsutomu Akama, Stephen J. Baker, Vincent S. Hernandez, Virginia Sanders, Yvonne Freund, Richard Kimura, Wei Bu, Karin M. Hold, Xiao-Song Lu,