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By G. Hasko

ISBN-10: 0849339995

ISBN-13: 9780849339998

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Extra info for Adenosine Receptors - Therapeutic Asps. for Inflamm., Immune Diseases

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3). 10 The A3AR affinity and efficacy of N6-arylethyl adenosines depend highly on stereochemistry, steric bulk, and ring constraints. 63 nM) but not rat A3AR. The dependence of the AR affinity and selectivity on phenyl ring substitution of N6-(1S,2R)-(2-phenyl-1-cyclopropyl)adenosine analogs were analyzed. A 3-nitrophenyl analog was resolved chromatographically into pure diastereomers, which displayed tenfold stereoselectivity in A3AR binding in favor of the 1S,2R isomer 15. A heteroaromatic group (3-thienyl) could substitute for the phenyl moiety of 14 with retention of high affinity of A3AR binding.

Lee, K. , Ring-constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5′-uronamide and 2′-deoxy modifications, Bioorg. Med. Chem. , 11, 1333, 2001. 27. Tchilibon, S. , (N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists, J. Med. , 48, 1745, 2005. 28. P. , 3′-Aminoadenosine-5′-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor, J. Med. , 46, 353, 2003. 29. Van Rompaey, P.

43, 2196, 2000. 26. Lee, K. , Ring-constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5′-uronamide and 2′-deoxy modifications, Bioorg. Med. Chem. , 11, 1333, 2001. 27. Tchilibon, S. , (N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists, J. Med. , 48, 1745, 2005. 28. P. , 3′-Aminoadenosine-5′-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor, J. Med. , 46, 353, 2003.

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Adenosine Receptors - Therapeutic Asps. for Inflamm., Immune Diseases by G. Hasko


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