- Discovery of 3,3′-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction
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In studies aimed toward identifying effective and safe inhibitors of kinase signaling cascades that underlie ischemia/reperfusion (I/R) injury, we synthesized a series of pteridines and pyridopyrazines. The design strategy was inspired by the examination
- Palanki, Moorthy S. S.,Dneprovskaia, Elena,Doukas, John,Fine, Richard M.,Hood, John,Kang, Xinshan,Lohse, Dan,Martin, Michael,Noronha, Glenn,Soll, Richard M.,Wrasidlo, Wolfgang,Yee, Shiyin,Zhu, Hong
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p. 4279 - 4294
(2008/02/13)
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- Discovery of 4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido [2,3-d]pyrimidine, an orally active, non-nucleoside adenosine kinase inhibitor
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Adenosine (ADO) is an endogenous homeostatic inhibitory neuromodulator that reduces cellular excitability at sites of tissue injury and inflammation. Inhibition of adenosine kinase (AK), the primary metabolic enzyme for ADO, selectively increases ADO concentrations at sites of tissue trauma and enhances the analgesic and antiinflammatory actions of ADO. Optimization of the high-throughput screening lead, 4-amino-7-aryl-substituted pteridine (5) (AK IC50 = 440 nM), led to the identification of compound 21 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido [2,3-d]pyrimidine, ABT-702), a novel, potent (AK IC50 = 1.7 nM) nonnucleoside AK inhibitor with oral activity in animal models of pain and inflammation.
- Lee,Jiang,Cowart,Gfesser,Perner,Ki Hwan Kim,Yu Gui Gu,Williams,Jarvis,Kowaluk,Stewart,Bhagwat
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p. 2133 - 2138
(2007/10/03)
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- On the Amination of Pteridines by Liquid Ammonia-Potassium Permanganate
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7-Phenyl, 7-(p-methoxyphenyl)-, 7-methyl-, 7-t-butyl-, 6,7-diphenyl-, 6,7-dimethyl- and 2-phenylpteridine are converted in good yields into their respective 4-amino compounds, when they are dissolved in liquid ammonia (-40 deg) and potassium permanganate
- Sladowska, H.,De Meester, J. W. G.,Plas, H. C. van der
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p. 477 - 480
(2007/10/02)
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- Diuretics
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Specific 4-amino pteridines carrying particular phenyl substituents in the 7-position and no substituents in the 2-position have been found to be excellent nonkaliuretic diuretics at doses of 30 to 500 mg/kg in warm-blooded animals.
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