Synthesis, CoMFA analysis, and receptor docking of 3, 5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists

…, N Forsyth, N Melman, X Ji, KA Jacobson

Index: Li, An-Hu; Moro, Stefano; Forsyth, Nancy; Melman, Neli; Ji, Xiao-Duo; Jacobson, Kenneth A. Journal of Medicinal Chemistry, 1999 , vol. 42, # 4 p. 706 - 721

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Citation Number: 201

Abstract

3, 5-Diacyl-2, 4-dialkyl-6-phenylpyridine derivatives have been found to be selective antagonists at both human and rat A3 adenosine receptors (Li et al. J. Med. Chem. 1998, 41, 3186-3201). In the present study, ring-constrained, fluoro, hydroxy, and other derivatives in this series have been synthesized and tested for affinity at adenosine receptors in radioligand binding assays. K i values at recombinant human and rat A3 adenosine ...