Hassler, Carla; Zhang, Yanan; Gilmour, Brian; Graf, Tyler; Fennell, Timothy; Snyder, Rodney; Deschamps, Jeffrey R.; Reinscheid, Rainer K.; Garau, Celia; Runyon, Scott P. published the artcile< Identification of Neuropeptide S Antagonists: Structure-Activity Relationship Studies, X-ray Crystallography, and in Vivo Evaluation>, Formula: C19H34O2, the main research area is diphenyltetrahydro oxazolo pyrazinone derivative preparation structure neuropeptide S antagonist.
Modulation of the neuropeptide S (NPS) system has been linked to a variety of CNS disorders such as panic disorder, anxiety, sleeping disorders, asthma, obesity, PTSD, and substance abuse. In this study, a series of diphenyltetrahydro-1H-oxazolo[3,4-α]pyrazin-3(5H)-ones were synthesized and evaluated for antagonist activity at the neuropeptide S receptor. The absolute configuration was determined by chiral resolution of the key synthetic intermediate, followed by anal. of one of the individual enantiomers by X-ray crystallog. The R isomer was then converted to a biol. active compound (34) that had a Ke of 36 nM. The most potent compound displayed enhanced aqueous solubility compared with the prototypical antagonist SHA-68 and demonstrated favorable pharmacokinetic properties for behavioral assessment. In vivo anal. in mice indicated a significant blockade of NPS induced locomotor activity at an i.p. dose of 50 mg/kg. This suggests that analogs having improved drug-like properties will facilitate more detailed studies of the neuropeptide S receptor system.
ACS Chemical Neuroscience published new progress about Central nervous system agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Formula: C19H34O2.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics