Synthesis and anthelmintic properties of arylquinolines with activity against drug-resistant nematodes

Sharon Rossiter; Jean Marie Péron; Philip J. Whitfield; Keith Jones

doi:10.1016/j.bmcl.2005.07.044

Synthesis and anthelmintic properties of arylquinolines with activity against drug-resistant nematodes

Sharon Rossiter
, Jean Marie Péron
, Philip J. Whitfield
, Keith Jones

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

Abstract

2,4-Disubstituted quinolines with additional substituents in positions 5-8 have been found to have anthelmintic properties. A number of 2,4-dimethoxy-6- or 8-arylquinolines have potent activity against the sheep nematode 'Haemonchus contortus', with LD99 values of the same order of magnitude as levamisole. These arylquinolines maintain their activity against levamisole-, ivermectin- and thiabendazole-resistant strains of 'H. contortus'.

Original language	English
Pages (from-to)	4806-4808
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	21
DOIs	https://doi.org/10.1016/j.bmcl.2005.07.044
Publication status	Published - 1 Nov 2005

Bibliographical note

Note: This work was supported by the Wellcome Trust.

Keywords

Quinolines
Suzuki coupling
Anthelmintics
Atanine
Chemistry

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10.1016/j.bmcl.2005.07.044

http://dx.doi.org/10.1016/j.bmcl.2005.07.044

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title = "Synthesis and anthelmintic properties of arylquinolines with activity against drug-resistant nematodes",

abstract = "2,4-Disubstituted quinolines with additional substituents in positions 5-8 have been found to have anthelmintic properties. A number of 2,4-dimethoxy-6- or 8-arylquinolines have potent activity against the sheep nematode 'Haemonchus contortus', with LD99 values of the same order of magnitude as levamisole. These arylquinolines maintain their activity against levamisole-, ivermectin- and thiabendazole-resistant strains of 'H. contortus'.",

keywords = "Quinolines, Suzuki coupling, Anthelmintics, Atanine, Chemistry",

author = "Sharon Rossiter and P{\'e}ron, \{Jean Marie\} and Whitfield, \{Philip J.\} and Keith Jones",

note = "Note: This work was supported by the Wellcome Trust.",

year = "2005",

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doi = "10.1016/j.bmcl.2005.07.044",

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T1 - Synthesis and anthelmintic properties of arylquinolines with activity against drug-resistant nematodes

AU - Rossiter, Sharon

AU - Péron, Jean Marie

AU - Whitfield, Philip J.

AU - Jones, Keith

N1 - Note: This work was supported by the Wellcome Trust.

PY - 2005/11/1

Y1 - 2005/11/1

N2 - 2,4-Disubstituted quinolines with additional substituents in positions 5-8 have been found to have anthelmintic properties. A number of 2,4-dimethoxy-6- or 8-arylquinolines have potent activity against the sheep nematode 'Haemonchus contortus', with LD99 values of the same order of magnitude as levamisole. These arylquinolines maintain their activity against levamisole-, ivermectin- and thiabendazole-resistant strains of 'H. contortus'.

AB - 2,4-Disubstituted quinolines with additional substituents in positions 5-8 have been found to have anthelmintic properties. A number of 2,4-dimethoxy-6- or 8-arylquinolines have potent activity against the sheep nematode 'Haemonchus contortus', with LD99 values of the same order of magnitude as levamisole. These arylquinolines maintain their activity against levamisole-, ivermectin- and thiabendazole-resistant strains of 'H. contortus'.

KW - Quinolines

KW - Suzuki coupling

KW - Anthelmintics

KW - Atanine

KW - Chemistry

UR - http://www.ncbi.nlm.nih.gov/pubmed/16165359

U2 - 10.1016/j.bmcl.2005.07.044

DO - 10.1016/j.bmcl.2005.07.044

M3 - Article

C2 - 16165359

SN - 0960-894X

VL - 15

SP - 4806

EP - 4808

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 21

ER -

Synthesis and anthelmintic properties of arylquinolines with activity against drug-resistant nematodes

Abstract

Bibliographical note

Keywords

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