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Bioorg Med Chem Lett. 2011 Apr 1;21(7):1933-6. doi: 10.1016/j.bmcl.2011.02.053. Epub 2011 Feb 17.

Discovery of benzothiazole-based adenosine A2B receptor antagonists with improved A2A selectivity.

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Roche Research Center, Hoffmann-La Roche, Inc, Nutley, NJ 07110, USA.


The highly potent but modestly selective N-(2-amino-4-methoxy-benzothiazol-7-yl)-N-ethyl-acetamide derivative 2 was selected as the starting point for the design of novel selective A(2B) antagonists, due to its excellent potency, and good drug-like properties. A series of compounds containing nonaromatic amides or ureas of five- or six-membered rings, and also bearing an m-trifluoromethyl-phenyl group (shown to impart superior potency) was prepared and evaluated for their selectivity against the A(2A) and A(1) receptors. This work resulted in the identification of compound 30, with excellent potency and high selectivity against both A(2A) and A(1) receptors.

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