The discovery of a selective, high affinity A 2B adenosine receptor antagonist for the potential treatment of asthma

…, R Kalla, T Perry, V Palle, V Varkhedkar, D Xiao…

Index: Zablocki, Jeff; Kalla, Rao; Perry, Thao; Palle, Venkata; Varkhedkar, Vaibhav; Xiao, Dengming; Piscopio, Anthony; Maa, Tenning; Gimbel, Art; Hao, Jia; Chu, Nancy; Leung, Kwan; Zeng, Dewan Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 3 p. 609 - 612 Title/Abstract View citing articles Show Details Elzein, Elfatih; Ibrahim, Prabha; Koltun, Dmitry O.; Rehder, Ken; Shenk, Kevin D.; Marquart, Timothy A.; Jiang, Bob; Li, Xiaofen; Natero, Reina; Li, Yuan; Nguyen, Marie; Kerwar, Suresh; Chu, Nancy; Soohoo, Daniel; Hao, Jia; Maydanik, Victoria Y.; Lustig, David A.; Zeng, Dewan; Leung, Kwan; Zablocki, Jeff A. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 24 p. 6017 - 6021

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Citation Number: 53

Abstract

Adenosine has been suggested to play a role in asthma, possibly via activation of A2B adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A2B AdoR antagonist that resulted in the discovery of CVT-5440, a high affinity A2B AdoR antagonist with good selectivity (A2B AdoR Ki= 50nM, selectivity A1> 200: A2A> 200: A3> 167).