1. Pyridopyrimidine analogues as novel adenosine kinase inhibitors
- Author
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John R. Koenig, Elizabeth A. Kowaluk, Karen M. Alexander, Andrew O. Stewart, Guo Zhu Zheng, Carol T. Wismer, Michael F. Jarvis, Yui Mao, Katharine L. Chu, Mark A. Matulenko, Richard J. Perner, Steve Muchmore, Ki H. Kim, Mei Qun Jiang, Kennan C. Marsh, Chih-Hung Lee, Haixia Yu, Shripad S. Bhagwat, Joseph P. Mikusa, John K. Pratt, Kathy L. Kohlhaas, Steve McGaraughty, and Arthur Gomtsyan
- Subjects
Models, Molecular ,Stereochemistry ,Morpholines ,Clinical Biochemistry ,Molecular Conformation ,Pharmaceutical Science ,Adenosine kinase ,Biochemistry ,Chemical synthesis ,Structure-Activity Relationship ,In vivo ,Drug Discovery ,Moiety ,Enzyme Inhibitors ,Molecular Biology ,Adenosine Kinase ,chemistry.chemical_classification ,biology ,Bicyclic molecule ,Organic Chemistry ,In vitro ,Enzyme ,Pyrimidines ,chemistry ,Enzyme inhibitor ,biology.protein ,Molecular Medicine - 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.
- Published
- 2001