373604-52-5Relevant academic research and scientific papers
Adenosine kinase inhibitors: Polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity
Zheng, Guo Zhu,Mao, Yue,Lee, Chih-Hung,Pratt, John K.,Koenig, John R.,Perner, Richard J.,Cowart, Marlon D.,Gfesser, Gregory A.,McGaraughty, Steve,Chu, Katharine L.,Zhu, Chang,Yu, Haixia,Kohlhaas, Kathy,Alexander, Karen M.,Wismer, Carol T.,Mikusa, Joseph,Jarvis, Michael F.,Kowaluk, Elizabeth A.,Stewart, Andrew O.
, p. 3041 - 3044 (2007/10/03)
We have discovered that polar 7-substituents of pyridopyrimidine derivatives affect not only whole cell AK inhibitory potency, but also selectivity in causing locomotor side effects in vivo animal models. We have identified compound, 1o, which has potent whole cell AK inhibitory potency, analgesic activity and minimal reduction of locomotor activity.
Pyridopyrimidine analogues as novel adenosine kinase inhibitors
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.
, p. 2071 - 2074 (2007/10/03)
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.
