By G. Hasko
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Extra info for Adenosine Receptors - Therapeutic Asps. for Inflamm., Immune Diseases
7 PYRAZOLOQUINOLINES The 2-aryl-pyrazolo [4,3-c] quinolin-4-one skeleton was recently reported as a template for selective A3AR antagonists. 0 nM. fm Page 32 Wednesday, May 24, 2006 3:00 PM 32 Adenosine Receptors were also identified in a library of compounds described earlier as a source of A3AR antagonists. 9 THIAZOLES AND THIADIAZOLES Thiazole and thiadiazole analogs 75–79 were first identified as a promising class of compounds after the screening of several 5- and 6-membered heterocyclic core templates to replace isoquinoline and quinazoline skeletons for new adenosine receptor antagonists.
42, 4473, 1999. 46. G. , Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors, Bioorg. Med. Chem. , 10, 209, 2000. 47. G. , Synthesis, biological activity, and molecular modeling investigation of new pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as human A3 adenosine receptor antagonists, J. Med. , 45, 770, 2002. 48. Maconi, A. , Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A3 adenosine receptor antagonist, J.
Selective agonists are in clinical trials for the treatment of rheumatoid arthritis and cancer. Selective antagonists are in preclinical testing for the treatment of glaucoma. In addition to the potential of directly acting orthosteric ligands, modulation of the ARs allosterically is a promising line of inquiry. The approach of genetic therapy with neoceptors could further achieve organ or tissue selectivity in the future. V. Joshi thanks Gilead Sciences, Foster City, CA, for financial support.
Adenosine Receptors - Therapeutic Asps. for Inflamm., Immune Diseases by G. Hasko