2-amino-N-pyrimidin-4-ylacetamides as A(2A) receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships

• Published in: Journal of medicinal chemistry Vol. 51; no. 6; pp. 1730 - 1739
• Main Authors: Slee, Deborah H., Moorjani, Manisha, Zhang, Xiaohu, Lin, Emily, Lanier, Marion C., Chen, Yongsheng, Rueter, Jaimie K., Lechner, Sandra M., Markison, Stacy, Malany, Siobhan, Joswig, Tanya, Samos, Mark, Gross, Raymond S., Williams, John P., Castro-Palomino, Julio C., Crespo, Maria I., Prat, Maria, Gual, Silvia, Diaz, Jose-Luis, Jalali, Kayvon, Sai, Yang, Zuo, Zhiyang, Yang, Chun, Wen, Jenny, O'Brien, Zhihong, Petroski, Robert, Saunders, John
• Format: Journal Article
• Language: English
• Published: WASHINGTON Amer Chemical Soc 27.03.2008
• Subjects: Chemistry, Medicinal; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Science & Technology; DYSKINESIA; HIGH-AFFINITY; ADENOSINE; K+ CHANNEL; BLOCKADE; ISTRADEFYLLINE; DOPAMINE D-4 RECEPTOR; NEUROPROTECTION; PARKINSONS-DISEASE; LEVODOPA

Previously we have described a series of novel A(2A) receptor antagonists with excellent water solubility. As described in the accompanying paper, the antagonists were first optimized to remove an unsubstituted furyl moiety, with the aim of avoiding the potential metabolic liabilities that can arise...