Novel 1, 3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A 2B adenosine receptor antagonists

…, X Li, T Perry, E Parkhill, V Palle, V Varkhedkar…

Index: Elzein, Elfatih; Kalla, Rao; Li, Xiaofen; Perry, Thao; Parkhill, Eric; Palle, Venkata; Varkhedkar, Vaibahv; Gimbel, Art; Zeng, Dewan; Lustig, David; Leung, Kwan; Zablocki, Jeff Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 2 p. 302 - 306

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Citation Number: 47

Abstract

A series of new 1, 3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as A2B-AdoR antagonists have been synthesized and evaluated for their binding affinities for the A2B, A1, A2A, and A3-AdoRs. 8-(1-((3-phenyl-1, 2, 4-oxadiazol-5-yl) methyl)-1H-pyrazol- 4-yl)-1, 3-dipropyl-1H-purine-2, 6 (3H, 7H)-dione (4) displayed high affinity (Ki= 1nM) and selectivity for the A2B-AdoR versus A1, A2A, and A3-AdoRs (A1/A2B, A2A/A2B, and A3/ ...