1053172-40-9Relevant academic research and scientific papers
A1 ADENOSINE RECEPTOR ALLOSTERIC ENHANCERS
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Page/Page column 49; 53, (2009/05/28)
The present invention relates generally to chemical compounds and methods for their use and preparation. In particular, the invention relates to chemical compounds which may possess useful therapeutic activity for treating conditions where the promotion of angiogensis (blood vessel formation) is beneficial, use of these compounds in therapy and the manufacture of medicaments as well as compositions containing these compounds.
5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers
Aurelio, Luigi,Figler, Heidi,Flynn, Bernard L.,Linden, Joel,Scammells, Peter J.
, p. 1319 - 1327 (2008/09/19)
Two series of 5-substituted 2-amino-4-(3-trifluoromethylphenyl)thiophenes were prepared and evaluated as allosteric enhancers at the A1 adenosine receptor (A1AR). In the 3-benzoyl series, a 5-phenyl group was found to confer the greatest potency (9a: ED50 = 2.1 μM, AE score = 18%). However, the analogue with no 5-substituent (6b: ED50 = 15.8 μM, AE score = 77%) proved to be the most efficacious. In the 3-ethoxycarbonyl series, the 5-(4-chlorophenyl) analogue was clearly the most potent and efficacious (9l: ED50 = 6.6 μM, AE score = 57%). The antagonist activity of all compounds was measured using a [3H]CPX competitive binding assay.
