Synthesis and biological activities of 4-phenyl-5-pyridyl-1, 3-thiazole derivatives as selective adenosine A3 antagonists

…, Y Arikawa, T Matsumoto, K Uga, N Kanzaki…

Index: Miwatashi, Seiji; Arikawa, Yasuyoshi; Matsumoto, Tatsumi; Uga, Keiko; Kanzaki, Naoyuki; Imai, Yumi N.; Ohkawa, Shigenori Chemical and Pharmaceutical Bulletin, 2008 , vol. 56, # 8 p. 1126 - 1137

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Citation Number: 12

Abstract

To investigate the potency of an adenosine A 3 receptor (A 3 AR) antagonist as an anti- asthmatic drug, a novel series of 4-phenyl-5-pyridyl-1, 3-thiazole derivatives was synthesized and evaluated in human adenosine A 1, A 2A and A 3 receptor and rat adenosine A 3 receptor binding assays. From investigation of the SAR study, compound 7af was identified as a highly potent human and rat A 3 AR antagonist. This compound ...