1373883-16-9Relevant academic research and scientific papers
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.
Preparation method for synthesizing n-heterocyclic carbine from chiral amino acid ester or hydrochloride
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Paragraph 0051-0055, (2019/07/05)
The invention discloses a preparation method for synthesizing n-heterocyclic carbine from a chiral amino acid ester or hydrochloride, the amino acid ester or a hydrochloride compound are taken as theraw materials to have an acylation reaction with alpha-c
Diastereoselective synthesis of novel 5-substituted morpholine-3-phosphonic acids: Further exploitation of N-acyliminium intermediates
Bonilla-Landa, Israel,Viveros-Ceballos, José Luis,Ordó?ez, Mario
, p. 485 - 487 (2014/05/06)
The first diastereoselective total synthesis of 5-substituted morpholine-3-phosphonic acids is reported. The principal feature of the synthesis is the introduction of a dimethyl phosphonate group into 5-substituted morpholin-3-ones. The procedure is based
