Exploring the potential of xanthene derivatives as trypanothione reductase inhibitors and chloroquine potentiating agents

Kelly Chibale; Mark Visser; Donelly van Schalkwyk; Peter J. Smith; Ahilan Saravanamuthu; Alan H. Fairlamb

doi:10.1016/S0040-4020(03)00240-0

Exploring the potential of xanthene derivatives as trypanothione reductase inhibitors and chloroquine potentiating agents

Kelly Chibale (Lead / Corresponding author), Mark Visser, Donelly van Schalkwyk, Peter J. Smith, Ahilan Saravanamuthu, Alan H. Fairlamb

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

188 Citations (Scopus)

Abstract

Xanthene derivatives were synthesized and evaluated for their potential as trypanothione reductase (TryR) inhibitors and chloroquine (CQ) potentiating agents. Some derivatives displayed inhibitory activity against TryR comparable to known tricyclic anti-depressants. On the other hand a number of derivatives increased CQ accumulation and potentiating effects in a resistant strain of Plasmodium falciparum with one compound also displaying strong intrinsic antimalarial activity.

Original language	English
Pages (from-to)	2289-2296
Number of pages	8
Journal	Tetrahedron
Volume	59
Issue number	13
DOIs	https://doi.org/10.1016/S0040-4020(03)00240-0
Publication status	Published - 24 Mar 2003

Keywords

9,9-dimethylxanthenes
Chloroquine potentiating agents
Leishmaniasis
Malaria
Trypanosomiasis
Trypanothione reductase inhibitors

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

UN SDGs

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

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10.1016/S0040-4020(03)00240-0

Cite this

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title = "Exploring the potential of xanthene derivatives as trypanothione reductase inhibitors and chloroquine potentiating agents",

abstract = "Xanthene derivatives were synthesized and evaluated for their potential as trypanothione reductase (TryR) inhibitors and chloroquine (CQ) potentiating agents. Some derivatives displayed inhibitory activity against TryR comparable to known tricyclic anti-depressants. On the other hand a number of derivatives increased CQ accumulation and potentiating effects in a resistant strain of Plasmodium falciparum with one compound also displaying strong intrinsic antimalarial activity.",

keywords = "9,9-dimethylxanthenes, Chloroquine potentiating agents, Leishmaniasis, Malaria, Trypanosomiasis, Trypanothione reductase inhibitors",

author = "Kelly Chibale and Mark Visser and {van Schalkwyk}, Donelly and Smith, {Peter J.} and Ahilan Saravanamuthu and Fairlamb, {Alan H.}",

note = "Funding Information: We would like to thank The Wellcome Trust for an International Research Development Fellowship award to K. C. (grant number 052075/Z/97). Further financial support from the National Research Foundation of South Africa (K. C.) is gratefully acknowledged. A. H. F. is supported by the Wellcome Trust.",

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doi = "10.1016/S0040-4020(03)00240-0",

language = "English",

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pages = "2289--2296",

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T1 - Exploring the potential of xanthene derivatives as trypanothione reductase inhibitors and chloroquine potentiating agents

AU - Chibale, Kelly

AU - Visser, Mark

AU - van Schalkwyk, Donelly

AU - Smith, Peter J.

AU - Saravanamuthu, Ahilan

AU - Fairlamb, Alan H.

N1 - Funding Information: We would like to thank The Wellcome Trust for an International Research Development Fellowship award to K. C. (grant number 052075/Z/97). Further financial support from the National Research Foundation of South Africa (K. C.) is gratefully acknowledged. A. H. F. is supported by the Wellcome Trust.

PY - 2003/3/24

Y1 - 2003/3/24

N2 - Xanthene derivatives were synthesized and evaluated for their potential as trypanothione reductase (TryR) inhibitors and chloroquine (CQ) potentiating agents. Some derivatives displayed inhibitory activity against TryR comparable to known tricyclic anti-depressants. On the other hand a number of derivatives increased CQ accumulation and potentiating effects in a resistant strain of Plasmodium falciparum with one compound also displaying strong intrinsic antimalarial activity.

AB - Xanthene derivatives were synthesized and evaluated for their potential as trypanothione reductase (TryR) inhibitors and chloroquine (CQ) potentiating agents. Some derivatives displayed inhibitory activity against TryR comparable to known tricyclic anti-depressants. On the other hand a number of derivatives increased CQ accumulation and potentiating effects in a resistant strain of Plasmodium falciparum with one compound also displaying strong intrinsic antimalarial activity.

KW - 9,9-dimethylxanthenes

KW - Chloroquine potentiating agents

KW - Leishmaniasis

KW - Malaria

KW - Trypanosomiasis

KW - Trypanothione reductase inhibitors

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U2 - 10.1016/S0040-4020(03)00240-0

DO - 10.1016/S0040-4020(03)00240-0

M3 - Article

AN - SCOPUS:0037463811

SN - 0040-4020

VL - 59

SP - 2289

EP - 2296

JO - Tetrahedron

JF - Tetrahedron

IS - 13

ER -

Exploring the potential of xanthene derivatives as trypanothione reductase inhibitors and chloroquine potentiating agents

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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