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

Authors
Yun, Jun; Han, Minsoo; Song, Chiman; Cheon, Seung Hoon; Choi, Kihang; Hahn, Hoh-Gyu
Issue Date
2014-08-01
Publisher
Pergamon Press Ltd.
Citation
Bioorganic & Medicinal Chemistry Letters, v.24, no.15, pp.3234 - 3237
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. (C) 2014 Elsevier Ltd. All rights reserved.
Keywords
BUPROPION; COMBINATION; BUPROPION; COMBINATION; Depression; Antidepressant; Triple reuptake inhibitor; 3-Phenethylazetidines
ISSN
0960-894X
URI
https://pubs.kist.re.kr/handle/201004/126492
DOI
10.1016/j.bmcl.2014.06.026
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KIST Article > 2014
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