A novel series of positive modulators of the AMPA receptor: structure-based lead optimization

Craig Jamieson; Robert A. Campbell; Iain A. Cumming; Kevin J. Gillen; Jonathan Gillespie; Bert Kazemier; Michael Kiczun; Yvonne Lamont; Amanda J. Lyons; John K.F. Maclean; Frederic Martin; Elizabeth M. Moir; John A. Morrow; John Pantling; Zoran Rankovic; Lynn Smith

doi:10.1016/j.bmcl.2010.08.063

A novel series of positive modulators of the AMPA receptor: structure-based lead optimization

Craig Jamieson, Robert A. Campbell, Iain A. Cumming, Kevin J. Gillen, Jonathan Gillespie, Bert Kazemier, Michael Kiczun, Yvonne Lamont, Amanda J. Lyons, John K.F. Maclean, Frederic Martin, Elizabeth M. Moir, John A. Morrow, John Pantling, Zoran Rankovic, Lynn Smith

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Abstract

Starting from lead compound 1, we demonstrate how x-ray structural data can be used to understand SAR and expediently optimize bioavailability in a novel series of AMPA receptor modulators, furnishing 5 with improved bioavailability and robust in vivo activity.

Original language	English
Pages (from-to)	6072-6075
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2010.08.063
Publication status	Published - 15 Oct 2010

Keywords

AMPA receptor
ion channels
positive allosteric modulators
SBDD

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Jamieson, C., Campbell, R. A., Cumming, I. A., Gillen, K. J., Gillespie, J., Kazemier, B., Kiczun, M., Lamont, Y., Lyons, A. J., Maclean, J. K. F., Martin, F., Moir, E. M., Morrow, J. A., Pantling, J., Rankovic, Z., & Smith, L. (2010). A novel series of positive modulators of the AMPA receptor: structure-based lead optimization. Bioorganic and Medicinal Chemistry Letters, 20(20), 6072-6075. https://doi.org/10.1016/j.bmcl.2010.08.063

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title = "A novel series of positive modulators of the AMPA receptor: structure-based lead optimization",

abstract = "Starting from lead compound 1, we demonstrate how x-ray structural data can be used to understand SAR and expediently optimize bioavailability in a novel series of AMPA receptor modulators, furnishing 5 with improved bioavailability and robust in vivo activity.",

keywords = "AMPA receptor, ion channels, positive allosteric modulators, SBDD",

author = "Craig Jamieson and Campbell, {Robert A.} and Cumming, {Iain A.} and Gillen, {Kevin J.} and Jonathan Gillespie and Bert Kazemier and Michael Kiczun and Yvonne Lamont and Lyons, {Amanda J.} and Maclean, {John K.F.} and Frederic Martin and Moir, {Elizabeth M.} and Morrow, {John A.} and John Pantling and Zoran Rankovic and Lynn Smith",

year = "2010",

month = oct,

day = "15",

doi = "10.1016/j.bmcl.2010.08.063",

language = "English",

volume = "20",

pages = "6072--6075",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "20",

}

Jamieson, C, Campbell, RA, Cumming, IA, Gillen, KJ, Gillespie, J, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, AJ, Maclean, JKF, Martin, F, Moir, EM, Morrow, JA, Pantling, J, Rankovic, Z & Smith, L 2010, 'A novel series of positive modulators of the AMPA receptor: structure-based lead optimization', Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 20, pp. 6072-6075. https://doi.org/10.1016/j.bmcl.2010.08.063

TY - JOUR

T1 - A novel series of positive modulators of the AMPA receptor

T2 - structure-based lead optimization

AU - Jamieson, Craig

AU - Campbell, Robert A.

AU - Cumming, Iain A.

AU - Gillen, Kevin J.

AU - Gillespie, Jonathan

AU - Kazemier, Bert

AU - Kiczun, Michael

AU - Lamont, Yvonne

AU - Lyons, Amanda J.

AU - Maclean, John K.F.

AU - Martin, Frederic

AU - Moir, Elizabeth M.

AU - Morrow, John A.

AU - Pantling, John

AU - Rankovic, Zoran

AU - Smith, Lynn

PY - 2010/10/15

Y1 - 2010/10/15

N2 - Starting from lead compound 1, we demonstrate how x-ray structural data can be used to understand SAR and expediently optimize bioavailability in a novel series of AMPA receptor modulators, furnishing 5 with improved bioavailability and robust in vivo activity.

AB - Starting from lead compound 1, we demonstrate how x-ray structural data can be used to understand SAR and expediently optimize bioavailability in a novel series of AMPA receptor modulators, furnishing 5 with improved bioavailability and robust in vivo activity.

KW - AMPA receptor

KW - ion channels

KW - positive allosteric modulators

KW - SBDD

UR - http://www.scopus.com/inward/record.url?scp=77956906200&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2010.08.063

DO - 10.1016/j.bmcl.2010.08.063

M3 - Article

SN - 0960-894X

VL - 20

SP - 6072

EP - 6075

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 20

ER -

A novel series of positive modulators of the AMPA receptor: structure-based lead optimization

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Keywords

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