A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs

Paul M. O'Neill; Steve Ward; Neil G. Berry; J. Prince Jeyadevan; Giancarlo Biagini; Egbaleh Asadollaly; B. Kevin Park; Patrick G. Bray

doi:10.2174/156802606776743147

A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs

Paul M. O'Neill, Steve Ward, Neil G. Berry, J. Prince Jeyadevan, Giancarlo Biagini, Egbaleh Asadollaly, B. Kevin Park, Patrick G. Bray

Tropical Disease Biology

Research output: Contribution to journal › Review article › peer-review

109 Citations (Scopus)

Abstract

A broad overview is presented describing the current knowledge and the ongoing research concerning the 4-aminoquinolines (4AQ) as chemotherapeutic antimalarial agents. Included are discussions of mechanism of action, structure activity relationships (SAR), chemistry, metabolism and toxicity and parasite resistance mechanisms. In discussions of SAR, particular emphasis has been given to activity versus chloroquine resistant strains of Plasmodium falciparum. Promising new lead compounds undergoing development are described and an overview of physicochemical properties of chloroquine and amodiaquine analogues is also included.

Original language	English
Pages (from-to)	479-507
Number of pages	29
Journal	Current Topics in Medicinal Chemistry
Volume	6
Issue number	5
DOIs	https://doi.org/10.2174/156802606776743147
Publication status	Published - 17 May 2006

Keywords

Antimalarial
Chloroquine (CQ) resistance
Combinatorial chemistry
Drug-design
Drug-metabolism
Plasmodium falciparum
Plasmodium falciparum chloroquine resistance transporter (PfCRT)

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title = "A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs",

abstract = "A broad overview is presented describing the current knowledge and the ongoing research concerning the 4-aminoquinolines (4AQ) as chemotherapeutic antimalarial agents. Included are discussions of mechanism of action, structure activity relationships (SAR), chemistry, metabolism and toxicity and parasite resistance mechanisms. In discussions of SAR, particular emphasis has been given to activity versus chloroquine resistant strains of Plasmodium falciparum. Promising new lead compounds undergoing development are described and an overview of physicochemical properties of chloroquine and amodiaquine analogues is also included.",

keywords = "Antimalarial, Chloroquine (CQ) resistance, Combinatorial chemistry, Drug-design, Drug-metabolism, Plasmodium falciparum, Plasmodium falciparum chloroquine resistance transporter (PfCRT)",

author = "O'Neill, \{Paul M.\} and Steve Ward and Berry, \{Neil G.\} and Jeyadevan, \{J. Prince\} and Giancarlo Biagini and Egbaleh Asadollaly and Park, \{B. Kevin\} and Bray, \{Patrick G.\}",

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language = "English",

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T1 - A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs

AU - O'Neill, Paul M.

AU - Ward, Steve

AU - Berry, Neil G.

AU - Jeyadevan, J. Prince

AU - Biagini, Giancarlo

AU - Asadollaly, Egbaleh

AU - Park, B. Kevin

AU - Bray, Patrick G.

PY - 2006/5/17

Y1 - 2006/5/17

N2 - A broad overview is presented describing the current knowledge and the ongoing research concerning the 4-aminoquinolines (4AQ) as chemotherapeutic antimalarial agents. Included are discussions of mechanism of action, structure activity relationships (SAR), chemistry, metabolism and toxicity and parasite resistance mechanisms. In discussions of SAR, particular emphasis has been given to activity versus chloroquine resistant strains of Plasmodium falciparum. Promising new lead compounds undergoing development are described and an overview of physicochemical properties of chloroquine and amodiaquine analogues is also included.

AB - A broad overview is presented describing the current knowledge and the ongoing research concerning the 4-aminoquinolines (4AQ) as chemotherapeutic antimalarial agents. Included are discussions of mechanism of action, structure activity relationships (SAR), chemistry, metabolism and toxicity and parasite resistance mechanisms. In discussions of SAR, particular emphasis has been given to activity versus chloroquine resistant strains of Plasmodium falciparum. Promising new lead compounds undergoing development are described and an overview of physicochemical properties of chloroquine and amodiaquine analogues is also included.

KW - Antimalarial

KW - Chloroquine (CQ) resistance

KW - Combinatorial chemistry

KW - Drug-design

KW - Drug-metabolism

KW - Plasmodium falciparum

KW - Plasmodium falciparum chloroquine resistance transporter (PfCRT)

U2 - 10.2174/156802606776743147

DO - 10.2174/156802606776743147

M3 - Review article

SN - 1568-0266

VL - 6

SP - 479

EP - 507

JO - Current Topics in Medicinal Chemistry

JF - Current Topics in Medicinal Chemistry

IS - 5

ER -

A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs

Abstract

Keywords

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