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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Pyrimidine benzamide-based thrombopoietin receptor agonists
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
نویسندگان
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