121103-15-9Relevant articles and documents
Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists
Ameriks, Michael K.,Ao, Hong,Carruthers, Nicholas I.,Lord, Brian,Ravula, Suchitra,Rech, Jason C.,Savall, Brad M.,Wall, Jessica L.,Wang, Qi,Bhattacharya, Anindya,Letavic, Michael A.
, p. 257 - 261 (2016)
The synthesis, SAR, and preclinical characterization of a series of substituted 6,7-dihydro[1,2,4]triazolo[4,3]pyrazin-8(5H)-one P2X7 receptor antagonists are described. Optimized leads from this series comprise some of the most potent human P2X7R antagonists reported to date (IC50s 50 = 0.8 mg/kg).
P2X7 MODULATORS
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Paragraph 0126; 0147, (2014/09/30)
The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
Parallel synthesis of an oligomeric imidazole-4, 5-dicarboxamide library
Xu, Zhigang,DiCesare, John C.,Baures, Paul W.
supporting information; experimental part, p. 248 - 254 (2010/08/19)
A library of oligomeric compounds was synthesized based on the imidazole-4, 5-dicarboxylic acid scaffold along with amino acid esters and chiral diamines derived from amino acids. The final compounds incorporate nonpolar amino acids (Leu, Phe, Trp), polar amino acids (Ser, Asp, Arg), and neutral amino acids (Gly, Ala), and were designed to be useful in screening for inhibitors of protein-protein interactions. Many of the protected and deprotected oligomers show evidence of conformational isomers persistent at room temperature in aqueous solution. A total of 317 final oligomers, out of 441 targeted compounds, were obtained in high analytical purity and of sufficient quantity to submit them for high-throughput screening as part of the NIH Roadmap.