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

Yun, Jun; Han, Minsoo; Song, Chiman; Cheon, Seung Hoon; Choi, Kihang; Hahn, Hoh-Gyu

doi:10.1016/j.bmcl.2014.06.026

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

Yun, Jun;
Han, Minsoo;
Song, Chiman;
Cheon, Seung Hoon;
Choi, Kihang;
외 1명

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10

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10

초록

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.

키워드

Depression; Antidepressant; Triple reuptake inhibitor; 3-Phenethylazetidines; BUPROPION; COMBINATION

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

저자: Yun, Jun; Han, Minsoo; Song, Chiman; Cheon, Seung Hoon; Choi, Kihang; Hahn, Hoh-Gyu

DOI: 10.1016/j.bmcl.2014.06.026

발행일: 2014-08-01

유형: Article

저널명: Bioorganic & Medicinal Chemistry Letters

권: 24

호: 15

페이지: 3234 ~ 3237