Novel Phenyl-Substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 Antagonists with Robust Target Engagement in Rat Brain was written by Chrovian, Christa C.;Soyode-Johnson, Akinola;Ao, Hong;Bacani, Genesis M.;Carruthers, Nicholas I.;Lord, Brian;Nguyen, Leslie;Rech, Jason C.;Wang, Qi;Bhattacharya, Anindya;Letavic, Michael A.. And the article was included in ACS Chemical Neuroscience in 2016.Category: piperazines The following contents are mentioned in the article:
Novel 5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists were optimized to allow for good blood-brain barrier permeability and high P2X7 target engagement in the brain of rats. Compound I (huP2X7 IC50 = 9 nM; rat P2X7 IC50 = 42 nM) achieved 80% receptor occupancy for 6 h when dosed orally at 10 mg/kg in rats as measured by ex vivo radioligand binding autoradiog. Structure-activity relationships within this series are described, as well as in vitro ADME results. In vivo pharmacokinetic data for key compounds is also included. This study involved multiple reactions and reactants, such as tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3Category: piperazines).
tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.Category: piperazines
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics