169447-69-2Relevant articles and documents
Structure-Activity Relationship Studies on Oxazolo[3,4- a]pyrazine Derivatives Leading to the Discovery of a Novel Neuropeptide S Receptor Antagonist with Potent in Vivo Activity
Albanese, Valentina,Ruzza, Chiara,Marzola, Erika,Bernardi, Tatiana,Fabbri, Martina,Fantinati, Anna,Trapella, Claudio,Reinscheid, Rainer K.,Ferrari, Federica,Sturaro, Chiara,Calò, Girolamo,Amendola, Giorgio,Cosconati, Sandro,Pacifico, Salvatore,Guerrini, Remo,Preti, Delia
, p. 4089 - 4108 (2021/04/12)
Neuropeptide S modulates important neurobiological functions including locomotion, anxiety, and drug abuse through interaction with its G protein-coupled receptor known as neuropeptide S receptor (NPSR). NPSR antagonists are potentially useful for the treatment of substance abuse disorders against which there is an urgent need for new effective therapeutic approaches. Potent NPSR antagonists in vitro have been discovered which, however, require further optimization of their in vivo pharmacological profile. This work describes a new series of NPSR antagonists of the oxazolo[3,4-a]pyrazine class. The guanidine derivative 16 exhibited nanomolar activity in vitro and 5-fold improved potency in vivo compared to SHA-68, a reference pharmacological tool in this field. Compound 16 can be considered a new tool for research studies on the translational potential of the NPSergic system. An in-depth molecular modeling investigation was also performed to gain new insights into the observed structure-activity relationships and provide an updated model of ligand/NPSR interactions.
Synthesis of new polysubstituted piperazines and dihydro-2H-pyrazines by selective reduction of 2-oxo-piperazines
Reginato, Gianna,Credico, Barbara Di,Andreotti, Daniele,Mingardi, Anna,Paio, Alfredo,Donati, Daniele,Pezzati, Bernardo,Mordini, Alessandro
experimental part, p. 191 - 194 (2010/05/18)
New enantiomerically enriched 1,4,5-piperazines and 1,4,5-dihydro-2H-pyrazines have been prepared by reduction of the corresponding 2-oxo-piperazines. Selective reduction can be achieved by careful control of the reaction conditions using LiAlH4/sub
PIPERAZINE UREA DERIVATIVES AS MELANOCORTIN-4 RECEPTOR AGONISTS
-
Page 81, (2010/11/30)
Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders r