Structure–activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A 3 receptor antagonists

KY Jung, SK Kim, ZG Gao, AS Gross, N Melman…

Index: Jung, Kwan-Young; Kim, Soo-Kyung; Gao, Zhan-Guo; Gross, Ariel S.; Melman, Neli; Jacobson, Kenneth A.; Kim, Yong-Chul Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 3 p. 613 - 623

Full Text: HTML

Citation Number: 128

Abstract

4-(4-Methoxyphenyl)-2-aminothiazole and 3-(4-methoxyphenyl)-5-aminothiadiazole derivatives have been synthesized and evaluated as selective antagonists for human adenosine A3 receptors. A methoxy group in the 4-position of the phenyl ring and N-acetyl or propionyl substitutions of the aminothiazole and aminothiadiazole templates displayed great increases of binding affinity and selectivity for human adenosine A3 receptors. The ...