Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors

We report the synthesis of 3-phenethylazetidine derivatives 2 and their biological activities against 5-HT, NE and DA transporters as well as microsomal stability, CYP inhibition, and hERG inhibition profiles. Compound 2at showed most potent triple reuptake inhibitor with good selectivity as a candi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-08, Vol.24 (15), p.3234-3237
Hauptverfasser:	Yun, Jun, Han, Minsoo, Song, Chiman, Cheon, Seung Hoon, Choi, Kihang, Hahn, Hoh-Gyu
Format:	Artikel
Sprache:	eng
Schlagworte:	Azetidines - chemical synthesis Azetidines - chemistry Azetidines - pharmacology Biological Transport - drug effects Cytochrome P-450 Enzyme Inhibitors - chemical synthesis Cytochrome P-450 Enzyme Inhibitors - chemistry Cytochrome P-450 Enzyme Inhibitors - pharmacology Cytochrome P-450 Enzyme System - metabolism Ether-A-Go-Go Potassium Channels - antagonists & inhibitors Ether-A-Go-Go Potassium Channels - metabolism Humans Molecular Structure Neurotransmitter Uptake Inhibitors - chemical synthesis Neurotransmitter Uptake Inhibitors - chemistry Neurotransmitter Uptake Inhibitors - pharmacology Phenyl Ethers - chemical synthesis Phenyl Ethers - chemistry Phenyl Ethers - pharmacology Plasma Membrane Neurotransmitter Transport Proteins - antagonists & inhibitors Plasma Membrane Neurotransmitter Transport Proteins - metabolism Serotonin - metabolism Structure-Activity Relationship
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Zusammenfassung:	We report the synthesis of 3-phenethylazetidine derivatives 2 and their biological activities against 5-HT, NE and DA transporters as well as microsomal stability, CYP inhibition, and hERG inhibition profiles. Compound 2at showed most potent triple reuptake inhibitor with good selectivity as a candidate for depression.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2014.06.026