Synthesis and Biological Evaluation of a Selective N- and P/Q-Type Calcium Channel Agonist was written by Liang, Mary;Tarr, Tyler B.;Bravo-Altamirano, Karla;Valdomir, Guillermo;Rensch, Gabriel;Swanson, Lauren;DeStefino, Nicholas R.;Mazzarisi, Cara M.;Olszewski, Rachel A.;Wilson, Gabriela Mustata;Meriney, Stephen D.;Wipf, Peter. And the article was included in ACS Medicinal Chemistry Letters in 2012.COA of Formula: C8H8Cl2N4 This article mentions the following:
The acute effect of the potent cyclin-dependent kinase (cdk) inhibitor (R)-roscovitine on Ca2+ channels inspired the development of structural analogs as a potential treatment for motor nerve terminal dysfunction. On the basis of a versatile chlorinated purine scaffold, we have synthesized ca. 20 derivatives, I [R1 = n-Pr, Me, CHMe2, R2 = CH2Ph, CH(Ph)2, 3-pyridinylmethyl, etc.], and characterized their N-type Ca2+ channel agonist action. I were prepared by reacting 2,6-dichloro-9H-purine with R1X/K2CO3/DMSO (X = halo), followed by reaction with R2NH2/NEt2/BuOH, which gave the 4-chloro-6-amino derivatives; the final step consisted of treating the latter compounds with (R)-2-amino-1-butanol at 170°C. Agents that showed strong agonist effects were also characterized in a kinase panel for their off-target effects. Among several novel compounds with diminished cdk activity, we identified a new lead structure with a 4-fold improved N-type Ca2+ channel agonist effect and a 22-fold decreased cdk2 activity as compared to (R)-roscovitine. This compound was selective for agonist activity on N- and P/Q-type over L-type calcium channels. In the experiment, the researchers used many compounds, for example, 2,6-Dichloro-9-isopropyl-9H-purine (cas: 203436-45-7COA of Formula: C8H8Cl2N4).
2,6-Dichloro-9-isopropyl-9H-purine (cas: 203436-45-7) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).COA of Formula: C8H8Cl2N4
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics