Discovery of benzamide analogues as a novel class of 5-HT3 receptor agonists

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Discovery of benzamide analogues as a novel class of 5-HT3 receptor agonists. / Jørgensen, Charlotte Grube; Frølund, Bente Flensborg; Kehler, Jan; Jensen, Anders Asbjørn.

In: ChemMedChem, Vol. 6, No. 4, 04.04.2011, p. 725-736.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Jørgensen, CG, Frølund, BF, Kehler, J & Jensen, AA 2011, 'Discovery of benzamide analogues as a novel class of 5-HT3 receptor agonists', ChemMedChem, vol. 6, no. 4, pp. 725-736. https://doi.org/10.1002/cmdc.201000444

APA

Jørgensen, C. G., Frølund, B. F., Kehler, J., & Jensen, A. A. (2011). Discovery of benzamide analogues as a novel class of 5-HT3 receptor agonists. ChemMedChem, 6(4), 725-736. https://doi.org/10.1002/cmdc.201000444

Vancouver

Jørgensen CG, Frølund BF, Kehler J, Jensen AA. Discovery of benzamide analogues as a novel class of 5-HT3 receptor agonists. ChemMedChem. 2011 Apr 4;6(4):725-736. https://doi.org/10.1002/cmdc.201000444

Author

Jørgensen, Charlotte Grube ; Frølund, Bente Flensborg ; Kehler, Jan ; Jensen, Anders Asbjørn. / Discovery of benzamide analogues as a novel class of 5-HT3 receptor agonists. In: ChemMedChem. 2011 ; Vol. 6, No. 4. pp. 725-736.

Bibtex

@article{69d31274cc6d4021aa3fac8a04aea610,
title = "Discovery of benzamide analogues as a novel class of 5-HT3 receptor agonists",
abstract = "A 5-HT(3) receptor agonist based on a benzamide scaffold was identified in a screening of a small commercial compound library, and an elaborate SAR study originating from this hit was performed. The design, synthesis, and functional characterisation of benzamide analogues at the 5-HT(3) A receptor yielded substantial information concerning the analogues as 5-HT(3) receptor agonists. However, the potencies of the derived analogues were not significantly improved over that of the initial hit. The benzamide scaffold constitutes a novel type of 5-HT(3) receptor agonist, as it does not possess a positively charged functionality, which is essential for the binding of all orthosteric ligands to the receptor. Preliminary investigations suggest that the compounds may exert their effects on 5-HT(3) receptors by binding to an allosteric site in the receptor complex.",
keywords = "Former Faculty of Pharmaceutical Sciences",
author = "J{\o}rgensen, {Charlotte Grube} and Fr{\o}lund, {Bente Flensborg} and Jan Kehler and Jensen, {Anders Asbj{\o}rn}",
note = "Keywords: agonists, allosterism, benzamides, ion channels, serotonin type 3 receptors",
year = "2011",
month = apr,
day = "4",
doi = "10.1002/cmdc.201000444",
language = "English",
volume = "6",
pages = "725--736",
journal = "Farmaco",
issn = "1860-7179",
publisher = "Wiley - V C H Verlag GmbH & Co. KGaA",
number = "4",

}

RIS

TY - JOUR

T1 - Discovery of benzamide analogues as a novel class of 5-HT3 receptor agonists

AU - Jørgensen, Charlotte Grube

AU - Frølund, Bente Flensborg

AU - Kehler, Jan

AU - Jensen, Anders Asbjørn

N1 - Keywords: agonists, allosterism, benzamides, ion channels, serotonin type 3 receptors

PY - 2011/4/4

Y1 - 2011/4/4

N2 - A 5-HT(3) receptor agonist based on a benzamide scaffold was identified in a screening of a small commercial compound library, and an elaborate SAR study originating from this hit was performed. The design, synthesis, and functional characterisation of benzamide analogues at the 5-HT(3) A receptor yielded substantial information concerning the analogues as 5-HT(3) receptor agonists. However, the potencies of the derived analogues were not significantly improved over that of the initial hit. The benzamide scaffold constitutes a novel type of 5-HT(3) receptor agonist, as it does not possess a positively charged functionality, which is essential for the binding of all orthosteric ligands to the receptor. Preliminary investigations suggest that the compounds may exert their effects on 5-HT(3) receptors by binding to an allosteric site in the receptor complex.

AB - A 5-HT(3) receptor agonist based on a benzamide scaffold was identified in a screening of a small commercial compound library, and an elaborate SAR study originating from this hit was performed. The design, synthesis, and functional characterisation of benzamide analogues at the 5-HT(3) A receptor yielded substantial information concerning the analogues as 5-HT(3) receptor agonists. However, the potencies of the derived analogues were not significantly improved over that of the initial hit. The benzamide scaffold constitutes a novel type of 5-HT(3) receptor agonist, as it does not possess a positively charged functionality, which is essential for the binding of all orthosteric ligands to the receptor. Preliminary investigations suggest that the compounds may exert their effects on 5-HT(3) receptors by binding to an allosteric site in the receptor complex.

KW - Former Faculty of Pharmaceutical Sciences

U2 - 10.1002/cmdc.201000444

DO - 10.1002/cmdc.201000444

M3 - Journal article

C2 - 21246737

VL - 6

SP - 725

EP - 736

JO - Farmaco

JF - Farmaco

SN - 1860-7179

IS - 4

ER -

ID: 33253259