Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 12, Issue 12, Pages 1563-1566Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(02)00236-6
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- NHLBI NIH HHS [R01-HL56111] Funding Source: Medline
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This report describes the synthesis and structure-activity relationships of a new class of A(1) adenosine receptor agonist allosteric enhancers, 2-aminothiazolium salts. The EC50 of compounds 6a, 6b, 7, and 8 were 0.3, 4.5, 3.8, and 1.2 muM, substantially lower than that of the 'Gold Standard' 2-amino-3-benzoyl thiophene (PD 81,723), which has an EC50 of 38 muM. (C) 2002 Elsevier Science Ltd. All rights reserved.
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