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2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability |
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| Authors: | Moorjani Manisha Zhang Xiaohu Chen Yongsheng Lin Emily Rueter Jaimie K Gross Raymond S Lanier Marion C Tellew John E Williams John P Lechner Sandra M Malany Siobhan Santos Mark Ekhlassi Paddi Castro-Palomino Julio C Crespo María I Prat Maria Gual Silvia Díaz José-Luis Saunders John Slee Deborah H |
| Institution: | Department of Medicinal Chemistry, Neurocrine Biosciences, 12790 El Camino Real, San Diego, CA 92130, USA. |
| Abstract: | In this report, the design and synthesis of a series of pyrimidine based adenosine A(2A) antagonists are described. The strategy and outcome of expanding SAR exploration to attenuate hERG and improve selectivity over A(1) are discussed. Compound 33 exhibited excellent potency, selectivity over A(1), and reduced hERG liability. |
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