کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365883 | 981575 | 2007 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Pyrimidine benzamide-based thrombopoietin receptor agonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A series of pyrimidine benzamide-based thrombopoietin receptor agonists is described. The lead molecule contains a 2-amino-5-unsubstituted thiazole, a group that has been associated with idiosyncratic toxicity. The potential for metabolic oxidation at C-5 of the thiazole, the likely source of toxic metabolites, was removed by substitution at C-5 or by replacing the thiazole with a thiadiazole. Potency in the series was improved by modifying the substituents on the pyrimidine and/or on the thiazole or thiadiazole pendant aryl ring. In vivo examination revealed that compounds from the series are not highly bioavailable. This is attributed to low solubility and poor permeability.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 19, 1 October 2007, Pages 5447–5454
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 19, 1 October 2007, Pages 5447–5454
نویسندگان
Lawrence A. Reiter, Chakrapani Subramanyam, Emilio J. Mangual, Christopher S. Jones, Marc I. Smeets, William H. Brissette, Sandra P. McCurdy, Paul D. Lira, Robert G. Linde, Qifang Li, Fangning Zhang, Amy S. Antipas, Laura C. Blumberg, Jonathan L. Doty,