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
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 14, 15 July 2010, Pages 4140-4146
نویسندگان
Adrian Wai-Hing Cheung, John Brinkman, Fariborz Firooznia, Alexander Flohr, Joseph Grimsby, Mary Lou Gubler, Kevin Guertin, Rachid Hamid, Nicholas Marcopulos, Roger D. Norcross, Lida Qi, Gwendolyn Ramsey, Jenny Tan, Yang Wen, Ramakanth Sarabu,