title: Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.
abstract: 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.
authors: Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea; Department of Chemistry, Research Institute for Natural Sciences, Korea University, Seoul 136-701, Republic of Korea.
authors: Jun
authors: J
authors: Yun
authors: Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea.
authors: Minsoo
authors: M
authors: Han
authors: Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea.
authors: Chiman
authors: C
authors: Song
authors: College of Pharmacy, Chonnam National University, Gwangju 500-757, Republic of Korea.
authors: Seung Hoon
authors: SH
authors: Cheon
authors: Department of Chemistry, Research Institute for Natural Sciences, Korea University, Seoul 136-701, Republic of Korea.
authors: Kihang
authors: K
authors: Choi
authors: Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea. Electronic address: hghahn@kist.re.kr.
authors: Hoh-Gyu
authors: HG
authors: Hahn
mesh_terms: D001384:Azetidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001692:Biological Transport / Q000187:drug effects; D065607:Cytochrome P-450 Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D051638:Ether-A-Go-Go Potassium Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D015394:Molecular Structure; D014179:Neurotransmitter Uptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010647:Phenyl Ethers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D050480:Plasma Membrane Neurotransmitter Transport Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012701:Serotonin / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: C000595732:3-(2-(4-chloro-3-fluorophenyl)-2-(3-fluorophenoxy)ethyl)azetidine; D001384:Azetidines; D065607:Cytochrome P-450 Enzyme Inhibitors; D051638:Ether-A-Go-Go Potassium Channels; D014179:Neurotransmitter Uptake Inhibitors; D010647:Phenyl Ethers; D050480:Plasma Membrane Neurotransmitter Transport Proteins; D012701:Serotonin; D003577:Cytochrome P-450 Enzyme System
keywords: 3-Phenethylazetidines; Antidepressant; Depression; Triple reuptake inhibitor