New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation
| Autor: | Maria Grazia Mamolo, Maurizio Romano, Daniele Zampieri, Renzo Menegazzi |
|---|---|
| Přispěvatelé: | Zampieri, Daniele, Romano, Maurizio, Menegazzi, Renzo, Mamolo, Maria Grazia |
| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Sigma receptors (σR) Cytotoxicity Clinical Biochemistry Sigma receptor Pharmaceutical Science Ligands Biochemistry Alkylacetamide derivative 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Piperidines Cell Line Tumor Drug Discovery Affinity and selectivity Alkylacetamide derivatives Humans Receptors sigma Molecular Biology Cholesterol biosynthesis Organic Chemistry 030104 developmental biology chemistry 030220 oncology & carcinogenesis Molecular Medicine Piperidine |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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