Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor was written by Helal, Christopher J.;Arnold, Eric P.;Boyden, Tracey L.;Chang, Cheng;Chappie, Thomas A.;Fennell, Kimberly F.;Forman, Michael D.;Hajos, Mihaly;Harms, John F.;Hoffman, William E.;Humphrey, John M.;Kang, Zhijun;Kleiman, Robin J.;Kormos, Bethany L.;Lee, Che-Wah;Lu, Jiemin;Maklad, Noha;McDowell, Laura;Mente, Scot;O’Connor, Rebecca E.;Pandit, Jayvardhan;Piotrowski, Mary;Schmidt, Anne W.;Schmidt, Christopher J.;Ueno, Hirokazu;Verhoest, Patrick R.;Yang, Edward X.. And the article was included in Journal of Medicinal Chemistry in 2017.Synthetic Route of C4H5IN2 This article mentions the following:
Phosphodiesterase 2A (PDE2A) inhibitors have been reported to demonstrate in vivo activity in preclin. models of cognition. To more fully explore the biol. of PDE2A inhibition, we sought to identify potent PDE2A inhibitors with improved brain penetration as compared to current literature compounds Applying estimated human dose calculations while simultaneously leveraging synthetically enabled chem. and structure-based drug design has resulted in a highly potent, selective, brain penetrant compound 71 (PF-05085727) that effects in vivo biochem. changes commensurate with PDE2A inhibition along with behavioral and electrophysiol. reversal of the effects of NMDA antagonists in rodents. This data supports the ability of PDE2A inhibitors to potentiate NMDA signaling and their further development for clin. cognition indications. In the experiment, the researchers used many compounds, for example, 5-Iodo-1-methyl-1H-pyrazole (cas: 34091-51-5Synthetic Route of C4H5IN2).
5-Iodo-1-methyl-1H-pyrazole (cas: 34091-51-5) belongs to iodide derivatives. Organic iodides are organic compounds containing a carbon-iodine (C-I) bond. The carbon-iodine bond is weaker than other carbon-halogen bonds due to the poor electronegative nature of the iodine atom. The C–I bond is the weakest of the carbon–halogen bonds. These bond strengths correlate with the electronegativity of the halogen, decreasing in the order F > Cl > Br > I.Synthetic Route of C4H5IN2
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com