835871-98-2

Upstream product

• 59749-54-1 2-(hydroxymethyl)-4H-chromen-4-one 
• 18398-73-7 methyl 4-oxo-4H-chromene-2-carboxylate 
• 4940-39-0 acide chromone carboxylique-2 
• 98-59-9 p-toluenesulfonyl chloride 
• 116543-90-9 2-(hydroxymethyl)-2,3-dihydro-4H-chromen-4-one 

Relevant academic research and scientific papers

Synthesis and Structure-Activity Relationships of Triazaspirodecanone Derivatives as Nociceptin/Orphanin FQ Receptor Ligands

Several spiroxatrine derivatives were synthesized and evaluated as potential NOP receptor ligands. Structural modifications of the 1,4-benzodioxane moiety of spiroxatrine have been the focus of this research project. The structure-activity relationships that emerged indicate that the presence of an H-bond donor group (hydroxyl group) is more favorable for NOP activity when it is positioned α with respect to the CH2 linked to the 1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one portion. Moreover, cis diastereoisomers of the hydroxyl derivatives4 and 22 show a moderately higher degree of stereoselectivity than trans isomers. In particular, the spiropiperidine derivative cis-4 has submicromolar agonistic activity, and it will be the reference compound for the design and synthesis of new NOP agonists.

Synthesis and structure-activity relationships of 1-aralkyl-4- benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent σ ligands

In the attempt to define more accurately structure-affinity relationships for σ1 and σ2 ligands, we synthesized and tested on σ subtype receptors a series of aralkyl derivatives of 4-benzylpiperidine, in which the effect of modificat