کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371845 981857 2009 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Using the Golden Triangle to optimize clearance and oral absorption
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Using the Golden Triangle to optimize clearance and oral absorption
چکیده انگلیسی

The Golden Triangle is a visualization tool developed from in vitro permeability, in vitro clearance and computational data designed to aid medicinal chemists in achieving metabolically stable, permeable and potent drug candidates. Classifying compounds as permeable and stable and plotting molecular weight (MW) versus octanol:buffer (pH 7.4) distribution coefficients (log D) or estimated octanol:buffer (pH 7.4) distribution coefficients (elog D) reveals useful trends. Analysis of at least two orthogonal trends, such as permeability and clearance, can be extremely effective in balancing and optimizing multiple properties. In addition, molecular weight and log D impact potency-efficiency calculations, allowing potency, clearance and permeability to be optimized simultaneously.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 19, 1 October 2009, Pages 5560–5564
نویسندگان
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