Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors

Park, Jung-eun; Song, Chiman; Choi, Keehyun; Sim, Taebo; Moon, Bongjin; Roh, Eun Joo

doi:10.1016/j.bmcl.2013.08.062

상세 보기

Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors

Park, Jung-eun;
Song, Chiman;
Choi, Keehyun;
Sim, Taebo;
Moon, Bongjin;
외 1명

Citations

WEB OF SCIENCE

11

Citations

SCOPUS

11

초록

A series of 3,4-diarylpyrrolidin-2-one was designed, prepared and evaluated as triple reuptake inhibitors for antidepressant. Most compounds exhibited comparable in vitro efficacy as norepinephrine and dopamine transporter reuptake inhibitors. Especially, 2i showed better potency than GBR-12909 (IC50 = 14 - nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 mu M-85.6 nM) for three transporters. (C) 2013 Elsevier Ltd. All rights reserved.

키워드

Triple reuptake inhibitors; Monoamine; Reuptake; Depression; Antidepressant; Serotonin; Dopamine; Norepinephrine; Lactam; PHARMACOLOGICAL EVALUATION; MAJOR DEPRESSION; PROFILE; POTENT; AGENTS

제목: Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors

저자: Park, Jung-eun; Song, Chiman; Choi, Keehyun; Sim, Taebo; Moon, Bongjin; Roh, Eun Joo

DOI: 10.1016/j.bmcl.2013.08.062

발행일: 2013-10-15

유형: Article

저널명: Bioorganic and Medicinal Chemistry Letters

권: 23

호: 20

페이지: 5515 ~ 5518