Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.

@article{Slee2008IdentificationON,
  title={Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.},
  author={Deborah H Slee and Xiaohu Zhang and Manisha Moorjani and Emily Y. Lin and Marion C Lanier and Yongsheng Chen and Jaimie K Rueter and Sandra Lechner and Stacy Markison and Siobhan Malany and Tanya Joswig and Mark A Santos and Raymond S. Gross and John Patrick Williams and Julio Cesar Castro-Palomino and Mar{\'i}a I Crespo and Maria Dolors Prat and S{\'i}lvia Gual and J E Diaz and Jenny Wen and Zhihong O'Brien and John Saunders},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 3},
  pages={400-6}
}
Potent adenosine hA2A receptor antagonists are often accompanied by poor aqueous solubility, which presents issues for drug development. Herein we describe the early exploration of the structure-activity relationships of a lead pyrimidin-4-yl acetamide series to provide potent and selective 2-amino-N-pyrimidin-4-yl acetamides as hA2A receptor antagonists with excellent aqueous solubility. In addition, this series of compounds has demonstrated good bioavailability and in vivo efficacy in a… CONTINUE READING