1272306-01-0Relevant academic research and scientific papers
New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation
Zampieri, Daniele,Romano, Maurizio,Menegazzi, Renzo,Mamolo, Maria Grazia
, p. 3206 - 3209 (2018/08/24)
The sigma receptor (σR) family has been considered mysterious for a long time. In fact, the σ2R subtype has been cloned only recently, revealing its identity as TMEM97, a NPC1-binding protein involved in cholesterol biosynthesis and implicated in the pathogenesis of cancer and neurologic disorders. With the aim of developing new chemical entities gifted with σR affinity, herein we report the design and synthesis of new piperidine-based alkylacetamide derivatives with mixed affinity towards both σ1 and σ2R subtypes.
Synthesis and receptor binding studies of some new arylcarboxamide derivatives as sigma-1 ligands
Zampieri, Daniele,Laurini, Erik,Vio, Luciano,Golob, Samuel,Fermeglia, Maurizio,Pricl, Sabrina,Mamolo, Maria Grazia
, p. 1021 - 1025 (2014/03/21)
We describe here the synthesis and the binding interaction with σ1 and σ2 receptors of a series of new arylcarboxamide derivatives variously substituted on the aromatic portions. Maintaining a partial scaffold of a series of compounds previously synthesized by us, we evaluate the effect of the substitution on σ binding. The synthesized compounds have been tested to estimate their affinity and selectivity toward σ1 and σ2 receptors. Two out of 16 derivatives showed an interesting σ1 affinity (21.2 and 13.6 nM - compounds 2m and 2p) and a good selectivity (Ki(σ 2)/Ki(σ1) >140 and >40, respectively).
