Synthesis and antimalarial activity of new 3-arylquinoxaline-2-carbonitrile derivatives

Belén Zarranz; Andrés Jaso; Ignacio Aldana; Antonio Monge; Séverine Maurel; Eric Deharo; Valérie Jullian; Michel Sauvain

doi:10.1055/s-0031-1296926

Synthesis and antimalarial activity of new 3-arylquinoxaline-2-carbonitrile derivatives

Belén Zarranz
, Andrés Jaso
, Ignacio Aldana
, Antonio Monge
, Séverine Maurel
, Eric Deharo
, Valérie Jullian
, Michel Sauvain

University of Navarra
Université de Toulouse

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

58 Scopus citations

Abstract

New series of 3-arylquinoxaline-carbonitrile derivatives have been synthesized from various 5-substituted or 5,6-disubstituted benzofuroxanes and tested for their in vitro and in vivo activity against the erythrocytic development of Plasmodium falciparum strain with different chloroquine- resistance status. Quinoxaline 1,4-dioxide derivatives showed superior antimalarial activity in respect to reduced quinoxaline analogues. The best activity was observed with nonsubstituted quinoxaline 1,4-dioxides in positions 6 and 7 of the aromatic ring and with a hydrogen or chloro substituent in para position of the phenyl group.

Original language	English
Pages (from-to)	754-761
Number of pages	8
Journal	Arzneimittel-Forschung/Drug Research
Volume	55
Issue number	12
DOIs	https://doi.org/10.1055/s-0031-1296926
State	Published - 2005
Externally published	Yes

UN SDGs

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

SDG 3 Good Health and Well-being

Keywords

Antimalarial agents
Quinoxaline-carbonitrile derivatives, in vitro and in vivo studies, synthesis
β-Hernatin

Access to Document

10.1055/s-0031-1296926

Cite this

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title = "Synthesis and antimalarial activity of new 3-arylquinoxaline-2-carbonitrile derivatives",

abstract = "New series of 3-arylquinoxaline-carbonitrile derivatives have been synthesized from various 5-substituted or 5,6-disubstituted benzofuroxanes and tested for their in vitro and in vivo activity against the erythrocytic development of Plasmodium falciparum strain with different chloroquine- resistance status. Quinoxaline 1,4-dioxide derivatives showed superior antimalarial activity in respect to reduced quinoxaline analogues. The best activity was observed with nonsubstituted quinoxaline 1,4-dioxides in positions 6 and 7 of the aromatic ring and with a hydrogen or chloro substituent in para position of the phenyl group.",

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doi = "10.1055/s-0031-1296926",

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T1 - Synthesis and antimalarial activity of new 3-arylquinoxaline-2-carbonitrile derivatives

AU - Zarranz, Belén

AU - Jaso, Andrés

AU - Aldana, Ignacio

AU - Monge, Antonio

AU - Maurel, Séverine

AU - Deharo, Eric

AU - Jullian, Valérie

AU - Sauvain, Michel

PY - 2005

Y1 - 2005

N2 - New series of 3-arylquinoxaline-carbonitrile derivatives have been synthesized from various 5-substituted or 5,6-disubstituted benzofuroxanes and tested for their in vitro and in vivo activity against the erythrocytic development of Plasmodium falciparum strain with different chloroquine- resistance status. Quinoxaline 1,4-dioxide derivatives showed superior antimalarial activity in respect to reduced quinoxaline analogues. The best activity was observed with nonsubstituted quinoxaline 1,4-dioxides in positions 6 and 7 of the aromatic ring and with a hydrogen or chloro substituent in para position of the phenyl group.

AB - New series of 3-arylquinoxaline-carbonitrile derivatives have been synthesized from various 5-substituted or 5,6-disubstituted benzofuroxanes and tested for their in vitro and in vivo activity against the erythrocytic development of Plasmodium falciparum strain with different chloroquine- resistance status. Quinoxaline 1,4-dioxide derivatives showed superior antimalarial activity in respect to reduced quinoxaline analogues. The best activity was observed with nonsubstituted quinoxaline 1,4-dioxides in positions 6 and 7 of the aromatic ring and with a hydrogen or chloro substituent in para position of the phenyl group.

KW - Antimalarial agents

KW - Quinoxaline-carbonitrile derivatives, in vitro and in vivo studies, synthesis

KW - β-Hernatin

UR - https://www.scopus.com/pages/publications/29744447563

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DO - 10.1055/s-0031-1296926

M3 - Artículo

C2 - 16430030

AN - SCOPUS:29744447563

SN - 0004-4172

VL - 55

SP - 754

EP - 761

JO - Arzneimittel-Forschung/Drug Research

JF - Arzneimittel-Forschung/Drug Research

IS - 12

ER -

Synthesis and antimalarial activity of new 3-arylquinoxaline-2-carbonitrile derivatives

Abstract

UN SDGs

Keywords

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