The discovery of potent antagonists of NPBWR1 (GPR7) was written by Romero, F. Anthony;Hastings, Nicholas B.;Moningka, Remond;Guo, Zhiqiang;Wang, Ming;Di Salvo, Jerry;Lei, Ying;Trusca, Dorina;Deng, Qiaolin;Tong, Vincent;Terebetski, Jenna L.;Ball, Richard G.;Ujjainwalla, Feroze. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Synthetic Route of C10H12N4 This article mentions the following:
The synthesis and evaluation of small mol. antagonists of the G protein-coupled receptor NPBWR1 (GPR7) are reported for the first time. [4-(5-Chloropyridin-2-yl)piperazin-1-yl][(1S,2S,4R)-4-{[(1R)-1-(4-methoxyphenyl)ethyl]amino}-2-(thiophen-3-yl)cyclohexyl]methanone (I) emerged as a hit from a high-throughput screen. Examination of substituents that focused on replacing the 5-chloropyridine and 4-methoxybenzylamino groups of I led to the identification of compounds that exhibited subnanomolar potencies as low as 660 pM {II [X = NH]} in the functional assay and 200 pM in the binding assay {II [X = O]}. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Synthetic Route of C10H12N4).
6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Synthetic Route of C10H12N4
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics