Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part II was written by Das, Sanjib;Shelke, Dnyaneshwar E.;Harde, Rajendra L.;Avhad, Vijayshree B.;Khairatkar-Joshi, Neelima;Gullapalli, Srinivas;Gupta, Praveen K.;Gandhi, Maulik N.;Bhateja, Deepak K.;Bajpai, Malini;Joshi, Ashwini A.;Marathe, Megha Y.;Gudi, Girish S.;Jadhav, Satyawan B.;Mahat, Mahamad Yunnus A.;Thomas, Abraham. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Name: 4-(2-Chloropyrimidin-4-yl)morpholine This article mentions the following:
We report the design and synthesis of novel pyrrolo[3,2-b]quinoline containing heteroarene ethers as PDE10A inhibitors with good to excellent potency, selectivity and metabolic stability. Further optimization of this primary series resulted in the identification of 1-methyl-3-(4-{[3-(pyridine-4-yl)pyrazin-2-yl]oxy}phenyl)-1H-pyrrolo[3,2-b]pyridine (I) with good hPDE10A potency (IC50: 6.3 nM), excellent selectivity over other related PDEs, and desirable physicochem. properties. The compound exhibited high peripheral and adequate brain levels upon oral dosing in rodents. The compound also showed excellent efficacy in multiple preclin. animal models related to psychiatric disorders, particularly schizophrenia. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Name: 4-(2-Chloropyrimidin-4-yl)morpholine).
4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Name: 4-(2-Chloropyrimidin-4-yl)morpholine
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia