Pyridopyrimidine analogues as novel adenosine kinase inhibitors

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 bioavailab...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-08, Vol.11 (16), p.2071-2074
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Kinase - antagonists & inhibitors Adenosine Kinase - metabolism Analgesics Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Medical sciences Models, Molecular Molecular Conformation Morpholines - chemistry Morpholines - pharmacology Neuropharmacology Pharmacology. Drug treatments Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Structure-Activity Relationship
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Zusammenfassung:	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. A novel series of pyridopyrimidine analogues 9 was identified as potent adenosine kinase inhibitors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00375-4