Gomez, Laurent published the artcileDesign and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders, Synthetic Route of 24415-66-5, the main research area is triazolopyrimidine preparation PDE2a inhibitor SAR memory disorder treatment.
A series of potent and selective [1,2,4]triazolo[1,5-a]pyrimidine PDE2a inhibitors is reported. The design and improvement of the binding properties of this series was achieved using X-ray crystal structures in conjunction with careful anal. of electronic and structural requirements for the PDE2a enzyme. One of the lead compounds, compound I (DNS-8254), was identified as a potent and highly selective PDE2a enzyme inhibitor with favorable rat pharmacokinetic properties. Interestingly, the increased potency of compound I was facilitated by the formation of a halogen bond with the oxygen of Tyr827 present in the PDE2a active site. In vivo, compound I demonstrated significant memory enhancing effects in a rat model of novel object recognition. Taken together, these data suggest that compound I may be a useful tool to explore the pharmacol. of selective PDE2a inhibition.
Journal of Medicinal Chemistry published new progress about Memory disorders. 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, Synthetic Route of 24415-66-5.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics