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

Research output: Contribution to journalArticle

23 Citations (Scopus)

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.
LanguageEnglish
Pages6072-6075
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number20
DOIs
Publication statusPublished - 15 Oct 2010

Fingerprint

AMPA Receptors
Modulators
Biological Availability
Lead compounds
X-Rays
X rays
Lead

Keywords

  • AMPA receptor
  • ion channels
  • positive allosteric modulators
  • SBDD

Cite this

Jamieson, Craig ; Campbell, Robert A. ; Cumming, Iain A. ; Gillen, Kevin J. ; Gillespie, Jonathan ; Kazemier, Bert ; Kiczun, Michael ; Lamont, Yvonne ; Lyons, Amanda J. ; Maclean, John K.F. ; Martin, Frederic ; Moir, Elizabeth M. ; Morrow, John A. ; Pantling, John ; Rankovic, Zoran ; Smith, Lynn. / A novel series of positive modulators of the AMPA receptor : structure-based lead optimization. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 20. pp. 6072-6075.
@article{196cadb2943547ad828862a6c0cd22a3,
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 = "10",
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",
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

A novel series of positive modulators of the AMPA receptor : structure-based lead optimization. / Jamieson, Craig; Campbell, Robert A.; Cumming, Iain A.; Gillen, Kevin J.; Gillespie, Jonathan; Kazemier, Bert; Kiczun, Michael; Lamont, Yvonne; Lyons, Amanda J.; Maclean, John K.F.; Martin, Frederic; Moir, Elizabeth M.; Morrow, John A.; Pantling, John; Rankovic, Zoran; Smith, Lynn.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 20, 15.10.2010, p. 6072-6075.

Research output: Contribution to journalArticle

TY - JOUR

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

T2 - Bioorganic and Medicinal Chemistry Letters

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

VL - 20

SP - 6072

EP - 6075

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 20

ER -