Bioorganic and Medicinal Chemistry Letters p. 83 - 86 (2001)
Update date:2022-09-26
Topics:
Cowart, Marlon
Lee, Chih-Hung
Gfesser, Gregory A.
Bayburt, Erol K.
Bhagwat, Shripad S.
Stewart, Andrew O.
Yu, Haixia
Kohlhaas, Kathy L.
McGaraughty, Steve
Wismer, Carol T.
Mikusa, Joseph
Zhu, Chang
Alexander, Karen M.
Jarvis, Michael F.
Kowaluk, Elizabeth A.
The synthesis and SAR of a novel series of non-nucleoside pyridopyrimidine inhibitors of the enzyme adenosine kinase (AK) are described. It was found that pyridopyrimidines with a broad range of medium and large non-polar substituents at the 5-position potently inhibited AK activity. A narrower range of analogues was capable of potently inhibiting adenosine phosphorylation in intact cells indicating an enhanced ability of these analogues to penetrate cell membranes. Potent AK inhibitors were found to effectively reduce nociception in animal models of thermal hyperalgesia and persistent pain. (C) 2000 Elsevier Science Ltd.
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