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

121 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
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

Bibliographical note

Funding Information:
The Sandler Research Foundation and the NIH (AI053862).

Keywords

4-Aminoquinoline malaria

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

UN SDGs

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

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10.1016/j.bmcl.2004.12.037

Cite this

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title = "Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities",

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 - Sherrill, John

AU - Liou, Ally P.

AU - Weisman, Jennifer L.

AU - DeRisi, Joseph L.

AU - Guy, R. Kiplin

N1 - Funding Information: The Sandler Research Foundation and the NIH (AI053862).

PY - 2005/2/15

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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.

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JO - Bioorganic and Medicinal Chemistry Letters

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

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

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