کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10594986 981854 2010 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: Drug-like and non-xanthine based A2B adenosine receptor antagonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: Drug-like and non-xanthine based A2B adenosine receptor antagonists
چکیده انگلیسی
7-N-Acetamide-4-methoxy-2-aminobenzothiazole 4-fluorobenzamide (compound 1) was chosen as a drug-like and non-xanthine based starting point for the discovery of A2B receptor antagonists because of its slight selectivity against A1 and A2A receptors and modest A2B potency. SAR exploration of compound 1 described herein included modifications to the 7-N-acetamide group, substitution of the 4-methoxy group by halogens as well as replacement of the p-flouro-benzamide side chain. This work culminated in the identification of compound 37 with excellent A2B potency, modest selectivity versus A2A and A1 receptors, and good rodent PK properties.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 14, 15 July 2010, Pages 4140-4146
نویسندگان
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