کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10593505 | 981808 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors](/preview/png/10593505.png)
چکیده انگلیسی
11β-HSD1 is increasingly seen as an attractive target for the treatment of type II diabetes and other elements of the metabolic syndrome. In this program of work we describe how a series of neutral 2-thioalkyl-pyridine 11β-HSD1 inhibitors were optimized in terms of their pharmacokinetic properties to give compounds with excellent bioavailability in both rat and dog through a core change to pyrimidine. A potential reactive metabolite issue with 4-thioalkyl-pyrimidines was circumvented by a switch from sulfur to carbon substitution.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 21, 1 November 2012, Pages 6756-6761
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 21, 1 November 2012, Pages 6756-6761
نویسندگان
James S. Scott, Adrian L. Gill, Linda Godfrey, Sam D. Groombridge, Amanda Rees, John Revill, Paul Schofield, Pernilla Sörme, Andrew Stocker, John G. Swales, Paul R.O. Whittamore,