Inhibition of trypanothione reductase and glutathione reductase by ferrocenic 4-aminoquinoline ureas

Margaret A. L. Blackie; Ahilan Saravanamuthu; Alan H. Fairlamb; Kelly Chibale

Inhibition of trypanothione reductase and glutathione reductase by ferrocenic 4-aminoquinoline ureas

Margaret A. L. Blackie
, Ahilan Saravanamuthu
, Alan H. Fairlamb
, Kelly Chibale

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

Abstract

New ferrocenic 4-aminoquinoline urea compounds have been tested for inhibition of trypanothione reductase (TryR) and human glutathione reductase (GR). Several compounds were also tested in vitro against Leishmania donovani, Trypanosoma cruzi and Trypanosoma brucei rhodesiense. All compounds showed significant improvement in inhibition of TryR relative to chloroquine with the best compound showing an IC50 value of 2.4 mu M (Chloroquine IC50 = 47.6 mu M).

Original language	English
Pages (from-to)	52-60
Number of pages	9
Journal	ARKIVOC
Volume	2008
Issue number	vi
Publication status	Published - 2008

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Ferroquine
7-chloroquinoline
urea
in vitro
trypanothione reductase
ACTIVITY IN-VITRO
TRYPANOSOMA-CRUZI
CRITHIDIA-FASCICULATA
ANALOGS
ANTIPROTOZOAL
LEISHMANIA
QUINACRINE
DISCOVERY
MALARIA
DESIGN

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title = "Inhibition of trypanothione reductase and glutathione reductase by ferrocenic 4-aminoquinoline ureas",

abstract = "New ferrocenic 4-aminoquinoline urea compounds have been tested for inhibition of trypanothione reductase (TryR) and human glutathione reductase (GR). Several compounds were also tested in vitro against Leishmania donovani, Trypanosoma cruzi and Trypanosoma brucei rhodesiense. All compounds showed significant improvement in inhibition of TryR relative to chloroquine with the best compound showing an IC50 value of 2.4 mu M (Chloroquine IC50 = 47.6 mu M).",

keywords = "Ferroquine, 7-chloroquinoline, urea, in vitro, trypanothione reductase, ACTIVITY IN-VITRO, TRYPANOSOMA-CRUZI, CRITHIDIA-FASCICULATA, ANALOGS, ANTIPROTOZOAL, LEISHMANIA, QUINACRINE, DISCOVERY, MALARIA, DESIGN",

author = "Blackie, \{Margaret A. L.\} and Ahilan Saravanamuthu and Fairlamb, \{Alan H.\} and Kelly Chibale",

note = "Commemorative Issue in Honor of Prof. Torbjorn Norin on the occasion of his 75th anniversary",

year = "2008",

language = "English",

volume = "2008",

pages = "52--60",

journal = "ARKIVOC",

issn = "1551-7004",

publisher = "Arkat",

number = "vi",

}

TY - JOUR

T1 - Inhibition of trypanothione reductase and glutathione reductase by ferrocenic 4-aminoquinoline ureas

AU - Blackie, Margaret A. L.

AU - Saravanamuthu, Ahilan

AU - Fairlamb, Alan H.

AU - Chibale, Kelly

N1 - Commemorative Issue in Honor of Prof. Torbjorn Norin on the occasion of his 75th anniversary

PY - 2008

Y1 - 2008

N2 - New ferrocenic 4-aminoquinoline urea compounds have been tested for inhibition of trypanothione reductase (TryR) and human glutathione reductase (GR). Several compounds were also tested in vitro against Leishmania donovani, Trypanosoma cruzi and Trypanosoma brucei rhodesiense. All compounds showed significant improvement in inhibition of TryR relative to chloroquine with the best compound showing an IC50 value of 2.4 mu M (Chloroquine IC50 = 47.6 mu M).

AB - New ferrocenic 4-aminoquinoline urea compounds have been tested for inhibition of trypanothione reductase (TryR) and human glutathione reductase (GR). Several compounds were also tested in vitro against Leishmania donovani, Trypanosoma cruzi and Trypanosoma brucei rhodesiense. All compounds showed significant improvement in inhibition of TryR relative to chloroquine with the best compound showing an IC50 value of 2.4 mu M (Chloroquine IC50 = 47.6 mu M).

KW - Ferroquine

KW - 7-chloroquinoline

KW - urea

KW - in vitro

KW - trypanothione reductase

KW - ACTIVITY IN-VITRO

KW - TRYPANOSOMA-CRUZI

KW - CRITHIDIA-FASCICULATA

KW - ANALOGS

KW - ANTIPROTOZOAL

KW - LEISHMANIA

KW - QUINACRINE

KW - DISCOVERY

KW - MALARIA

KW - DESIGN

M3 - Article

SN - 1551-7004

VL - 2008

SP - 52

EP - 60

JO - ARKIVOC

JF - ARKIVOC

IS - vi

ER -

Inhibition of trypanothione reductase and glutathione reductase by ferrocenic 4-aminoquinoline ureas

Abstract

UN SDGs

Keywords

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