264880-77-5Relevant academic research and scientific papers
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents
Slee, Deborah H.,Chen, Yongsheng,Zhang, Xiaohu,Moorjani, Manisha,Lanier, Marion C.,Lin, Emily,Rueter, Jaimie K.,Williams, John P.,Lechner, Sandra M.,Markison, Stacy,Malany, Siobhan,Santos, Mark,Gross, Raymond S.,Jalali, Kayvon,Sai, Yang,Zuo, Zhiyang,Yang, Chun,Castro-Palomino, Julio C.,Crespo, María I.,Prat, Maria,Gual, Silvia,Díaz, José-Luis,Saunders, John
, p. 1719 - 1729 (2008/09/21)
Previously we have described a novel series of potent and selective A 2A receptor antagonists (e.g., 1) with excellent aqueous solubility.1 While these compounds are efficacious A2A antagonists in vivo, the presence of an
2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A2A antagonists with reduced hERG liability
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, Maria I.,Prat, Maria,Gual, Silvia,Diaz, Jose-Luis,Saunders, John,Slee, Deborah H.
, p. 1269 - 1273 (2008/09/18)
In this report, the design and synthesis of a series of pyrimidine based adenosine A2A antagonists are described. The strategy and outcome of expanding SAR exploration to attenuate hERG and improve selectivity over A1 are discussed.
