Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students

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

doi:10.1016/j.bmcl.2013.08.062

Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students

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

KU-KIST Graduate School of Converging Science and Technology

Research output: Contribution to journal › Article › peer-review

9 Citations (Scopus)

Abstract

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 (IC ₅₀ = 14 nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 μM-85.6 nM) for three transporters.

Original language	English
Pages (from-to)	5515-5518
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	23
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2013.08.062
Publication status	Published - 2013 Oct 15

Keywords

Antidepressant
Depression
Dopamine
Lactam
Monoamine
Norepinephrine
Reuptake
Serotonin
Triple reuptake inhibitors

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/j.bmcl.2013.08.062

Fingerprint

Dive into the research topics of 'Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students'. Together they form a unique fingerprint.

Cite this

Park, J. E., Song, C., Choi, K., Sim, T., Moon, B., & Roh, E. J. (2013). Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students. Bioorganic and Medicinal Chemistry Letters, 23(20), 5515-5518. https://doi.org/10.1016/j.bmcl.2013.08.062

Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students. / Park, Jung Eun; Song, Chiman; Choi, Keehyun et al.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 23, No. 20, 15.10.2013, p. 5515-5518.

Research output: Contribution to journal › Article › peer-review

Park, JE, Song, C, Choi, K, Sim, T, Moon, B & Roh, EJ 2013, 'Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students', Bioorganic and Medicinal Chemistry Letters, vol. 23, no. 20, pp. 5515-5518. https://doi.org/10.1016/j.bmcl.2013.08.062

@article{ea09ccb0a4cd4841817425760c284853,

title = "Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students",

abstract = "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 (IC 50 = 14 nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 μM-85.6 nM) for three transporters.",

keywords = "Antidepressant, Depression, Dopamine, Lactam, Monoamine, Norepinephrine, Reuptake, Serotonin, Triple reuptake inhibitors",

author = "Park, {Jung Eun} and Chiman Song and Keehyun Choi and Taebo Sim and Bongjin Moon and Roh, {Eun Joo}",

note = "Funding Information: This work was supported by the KIST Institutional Program (Grant No. 2E24090 ) from Korea Institute of Science and Technology and the Creative Fusion Research Program from Korea Research Council of Fundamental Science and Technology . ",

year = "2013",

month = oct,

day = "15",

doi = "10.1016/j.bmcl.2013.08.062",

language = "English",

volume = "23",

pages = "5515--5518",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "20",

}

TY - JOUR

T1 - Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students

AU - Park, Jung Eun

AU - Song, Chiman

AU - Choi, Keehyun

AU - Sim, Taebo

AU - Moon, Bongjin

AU - Roh, Eun Joo

N1 - Funding Information: This work was supported by the KIST Institutional Program (Grant No. 2E24090 ) from Korea Institute of Science and Technology and the Creative Fusion Research Program from Korea Research Council of Fundamental Science and Technology .

PY - 2013/10/15

Y1 - 2013/10/15

N2 - 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 (IC 50 = 14 nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 μM-85.6 nM) for three transporters.

AB - 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 (IC 50 = 14 nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 μM-85.6 nM) for three transporters.

KW - Antidepressant

KW - Depression

KW - Dopamine

KW - Lactam

KW - Monoamine

KW - Norepinephrine

KW - Reuptake

KW - Serotonin

KW - Triple reuptake inhibitors

UR - http://www.scopus.com/inward/record.url?scp=84884282193&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84884282193&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2013.08.062

DO - 10.1016/j.bmcl.2013.08.062

M3 - Article

C2 - 24012181

AN - SCOPUS:84884282193

SN - 0960-894X

VL - 23

SP - 5515

EP - 5518

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 20

ER -

Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this