کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369663 | 981784 | 2012 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Lead optimization of a sulfonylurea-based piperazine pyridazinone series of glucan synthase inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The structure–activity relationship studies of a novel sulfonylurea series of piperazine pyridazine-based small molecule glucan synthase inhibitors is described. The optimization of PK profiles within the series led to the discovery of several compounds with improved pharmacokinetic profiles which demonstrated in vitro potency against clinically relevant strains. However, the advancement of compounds from this series into a non-lethal systemic fungal infection model failed to show in vivo efficacy.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 14, 15 July 2012, Pages 4896–4899
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 14, 15 July 2012, Pages 4896–4899
نویسندگان
Andrew J. Zych, Sang Q. Lam, David M. Jenkins, R. Jason Herr, Pauline C. Ting, Joe F. Lee, Rongze Kuang, Heping Wu, David W. Kim, Robert G. Aslanian, Samuel Wainhaus, Todd A. Black, Anthony Cacciapuoti, Paul M. McNicholas, Yiming Xu, Scott S. Walker,