Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities

Peter B. Madrid; John Sherrill; Ally P. Liou; Jennifer L. Weisman; Joseph L. DeRisi; R. Kiplin Guy

doi:10.1016/j.bmcl.2004.12.037

Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities

Peter B. Madrid
, John Sherrill
, Ally P. Liou
, Jennifer L. Weisman
, Joseph L. DeRisi
, R. Kiplin Guy

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

122 Scopus citations

Abstract

A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2.

Original language	English (US)
Pages (from-to)	1015-1018
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	4
DOIs	https://doi.org/10.1016/j.bmcl.2004.12.037
State	Published - Feb 15 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

4-Aminoquinoline malaria

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10.1016/j.bmcl.2004.12.037

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abstract = "A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2.",

keywords = "4-Aminoquinoline malaria",

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AU - Madrid, Peter B.

AU - Sherrill, John

AU - Liou, Ally P.

AU - Weisman, Jennifer L.

AU - DeRisi, Joseph L.

AU - Guy, R. Kiplin

PY - 2005/2/15

Y1 - 2005/2/15

N2 - A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2.

AB - A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2.

KW - 4-Aminoquinoline malaria

UR - https://www.scopus.com/pages/publications/16244409252

UR - https://www.scopus.com/pages/publications/16244409252#tab=citedBy

U2 - 10.1016/j.bmcl.2004.12.037

DO - 10.1016/j.bmcl.2004.12.037

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SN - 0960-894X

VL - 15

SP - 1015

EP - 1018

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 4

ER -

Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities

Abstract

UN SDGs

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