So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Yang, Zhaohui; Li, Linlang; Zheng, Jiyue; Ma, Haikuo; Tian, Sheng; Li, Jiajun; Zhang, Hongjian; Zhen, Xuechu; Zhang, Xiaohu researched the compound: (S)-3-Methoxypyrrolidine( cas:120099-61-8 ).Quality Control of (S)-3-Methoxypyrrolidine.They published the article 《Identification of a New Series of Potent Adenosine A2A Receptor Antagonists Based on 4-Amino-5-carbonitrile Pyrimidine Template for the Treatment of Parkinson’s Disease》 about this compound( cas:120099-61-8 ) in ACS Chemical Neuroscience. Keywords: aminocarbonitrile pyrimidine preparation adenosine A2A receptor antagonist design antiparkinsonian; Adenosine receptor; GPCR; Parkinson’s disease; antagonist; lead identification. We’ll tell you more about this compound (cas:120099-61-8).
Adenosine receptor A2A antagonists have emerged as potential treatment for Parkinson’s disease in the past decade. The authors have recently reported a series of adenosine receptor antagonists using heterocycles as bioisosteres for a potentially unstable acetamide. These compounds, while showing excellent potency and ligand efficiency, suffered from moderate cytochrome P 450 inhibition and high clearance. Here the authors report a new series of adenosine receptor A2A antagonists based on a 4-amino-5-carbonitrile pyrimidine template. Compounds from this new template exhibit excellent potency and ligand efficiency with low cytochrome P 450 inhibition. Although the clearance remains moderate to high, the leading compound, when dosed orally as low as 3 mg/kg, demonstrated excellent efficacy in the haloperidol induced catalepsy rat model for Parkinson’s disease.
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Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia