Pyridopyrimidine analogues as novel adenosine kinase inhibitors

…, A Gomtsyan, MA Matulenko, Y Mao, JR Koenig…

Index: Zheng, Guo Zhu; Lee, Chih-Hung; Pratt, John K.; Perner, Richard J.; Jiang, Mei Qun; Gomtsyan, Arthur; Matulenko, Mark A.; Mao, Yui; Koenig, John R.; Kim, Ki H.; Muchmore, Steve; Yu, Haixia; Kohlhaas, Kathy; Alexander, Karen M.; McGaraughty, Steve; Chu, Katharine L.; Wismer, Carol T.; Mikusa, Joseph; Jarvis, Michael F.; Marsh, Kennan; Kowaluk, Elizabeth A.; Bhagwat, Shripad S.; Stewart, Andrew O. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 16 p. 2071 - 2074

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Citation Number: 24

Abstract

A novel series of pyridopyrimidine analogues 9 was identified as potent adenosine kinase inhibitors based on the SAR and computational studies. Substitution of the C7 position of the pyridopyrimidino core with C2′ substituted pyridino moiety increased the in vivo potency and enhanced oral bioavailability of these adenosine kinase inhibitors.