New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein

Louise Stevenson; Adriana A. S. Tavares; Aurelie Brunet; Fiona I. McGonagle; Deborah Dewar; Sally L. Pimlott; Andrew Sutherland

doi:10.1016/j.bmcl.2009.12.061

New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein

Louise Stevenson
, Adriana A. S. Tavares
, Aurelie Brunet
, Fiona I. McGonagle
, Deborah Dewar
, Sally L. Pimlott
, Andrew Sutherland^*

^*Corresponding author for this work

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

Abstract

With the aim of developing new SPECT imaging agents for the translocator protein (TSPO), a small library of iodinated quinoline-2-carboxamides have been prepared and tested for binding affinity with TSPO. N,N-Diethyl-3-iodomethyl-4-phenylquinoline-2-carboxamide was found to have excellent affinity (K(i) 12.0 nM), comparable to that of the widely used TSPO imaging agent PK11195. (c) 2009 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	954-957
Number of pages	4
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	20
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2009.12.061
Publication status	Published - 1 Feb 2010

Keywords / Materials (for Non-textual outputs)

SPECT
Imaging
Translocator protein
Quinoline-2-carboxamides
Heterocyclic synthesis
PERIPHERAL BENZODIAZEPINE-RECEPTOR
POSITRON-EMISSION-TOMOGRAPHY
CARBOXAMIDE DERIVATIVES
HIGH-AFFINITY
18 KDA
POTENTIAL RADIOLIGANDS
BINDING-SITES
LIGAND
PET
BRAIN

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10.1016/j.bmcl.2009.12.061

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title = "New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein",

abstract = "With the aim of developing new SPECT imaging agents for the translocator protein (TSPO), a small library of iodinated quinoline-2-carboxamides have been prepared and tested for binding affinity with TSPO. N,N-Diethyl-3-iodomethyl-4-phenylquinoline-2-carboxamide was found to have excellent affinity (K(i) 12.0 nM), comparable to that of the widely used TSPO imaging agent PK11195. (c) 2009 Elsevier Ltd. All rights reserved.",

keywords = "SPECT, Imaging, Translocator protein, Quinoline-2-carboxamides, Heterocyclic synthesis, PERIPHERAL BENZODIAZEPINE-RECEPTOR, POSITRON-EMISSION-TOMOGRAPHY, CARBOXAMIDE DERIVATIVES, HIGH-AFFINITY, 18 KDA, POTENTIAL RADIOLIGANDS, BINDING-SITES, LIGAND, PET, BRAIN",

author = "Louise Stevenson and Tavares, \{Adriana A. S.\} and Aurelie Brunet and McGonagle, \{Fiona I.\} and Deborah Dewar and Pimlott, \{Sally L.\} and Andrew Sutherland",

year = "2010",

month = feb,

day = "1",

doi = "10.1016/j.bmcl.2009.12.061",

language = "English",

volume = "20",

pages = "954--957",

journal = "Bioorganic \& Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier",

number = "3",

}

TY - JOUR

T1 - New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein

AU - Stevenson, Louise

AU - Tavares, Adriana A. S.

AU - Brunet, Aurelie

AU - McGonagle, Fiona I.

AU - Dewar, Deborah

AU - Pimlott, Sally L.

AU - Sutherland, Andrew

PY - 2010/2/1

Y1 - 2010/2/1

N2 - With the aim of developing new SPECT imaging agents for the translocator protein (TSPO), a small library of iodinated quinoline-2-carboxamides have been prepared and tested for binding affinity with TSPO. N,N-Diethyl-3-iodomethyl-4-phenylquinoline-2-carboxamide was found to have excellent affinity (K(i) 12.0 nM), comparable to that of the widely used TSPO imaging agent PK11195. (c) 2009 Elsevier Ltd. All rights reserved.

AB - With the aim of developing new SPECT imaging agents for the translocator protein (TSPO), a small library of iodinated quinoline-2-carboxamides have been prepared and tested for binding affinity with TSPO. N,N-Diethyl-3-iodomethyl-4-phenylquinoline-2-carboxamide was found to have excellent affinity (K(i) 12.0 nM), comparable to that of the widely used TSPO imaging agent PK11195. (c) 2009 Elsevier Ltd. All rights reserved.

KW - SPECT

KW - Imaging

KW - Translocator protein

KW - Quinoline-2-carboxamides

KW - Heterocyclic synthesis

KW - PERIPHERAL BENZODIAZEPINE-RECEPTOR

KW - POSITRON-EMISSION-TOMOGRAPHY

KW - CARBOXAMIDE DERIVATIVES

KW - HIGH-AFFINITY

KW - 18 KDA

KW - POTENTIAL RADIOLIGANDS

KW - BINDING-SITES

KW - LIGAND

KW - PET

KW - BRAIN

U2 - 10.1016/j.bmcl.2009.12.061

DO - 10.1016/j.bmcl.2009.12.061

M3 - Article

SN - 0960-894X

VL - 20

SP - 954

EP - 957

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 3

ER -

New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein

Abstract

Keywords / Materials (for Non-textual outputs)

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