Synthesis and biological activities of 4-N-(anilinyl-n-[oxazolyl])-7-chloroquinolines (n=3' or 4') against Plasmodium falciparum in in vitro models.

Erin E. Gordey; Paras N. Yadav; Marcus P. Merrin; Jill Davies; Steve Ward; Grant M.J. Woodman; Amber L. Sadowy; Todd G. Smith; Robert A. Gossage

doi:10.1016/j.bmcl.2011.05.131

Synthesis and biological activities of 4-N-(anilinyl-n-[oxazolyl])-7-chloroquinolines (n=3' or 4') against Plasmodium falciparum in in vitro models.

Erin E. Gordey
, Paras N. Yadav
, Marcus P. Merrin
, Jill Davies
, Steve Ward
, Grant M.J. Woodman
, Amber L. Sadowy
, Todd G. Smith
, Robert A. Gossage

Tropical Disease Biology

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

29 Citations (Scopus)

Abstract

The synthesis (Pd-mediated coupling strategy) and characterization (NMR, IR, elemental analysis, etc.) of a short series of quinoline-oxazole hybrid compounds has been carried out. These materials are found to be moderately active against Plasmodium falciparum in vitro, with activities in the sub-micromolar range, and to display acceptable cytotoxicity to mononuclear leukocytes. Chemical modification strategies, with the intention to increase the biological potency of this new class of anti-malarial agents, are discussed.

Original language	English
Pages (from-to)	4512-4515
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	15
DOIs	https://doi.org/10.1016/j.bmcl.2011.05.131
Publication status	Published - 1 Aug 2011

Keywords

Anti-malarial
IC
Oxazoline
Plasmodium falciparum
Pre-clinical evaluation
Toxicity

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10.1016/j.bmcl.2011.05.131

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Gordey, E. E., Yadav, P. N., Merrin, M. P., Davies, J., Ward, S., Woodman, G. M. J., Sadowy, A. L., Smith, T. G., & Gossage, R. A. (2011). Synthesis and biological activities of 4-N-(anilinyl-n-[oxazolyl])-7-chloroquinolines (n=3' or 4') against Plasmodium falciparum in in vitro models. Bioorganic and Medicinal Chemistry Letters, 21(15), 4512-4515. https://doi.org/10.1016/j.bmcl.2011.05.131

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title = "Synthesis and biological activities of 4-N-(anilinyl-n-[oxazolyl])-7-chloroquinolines (n=3' or 4') against Plasmodium falciparum in in vitro models.",

abstract = "The synthesis (Pd-mediated coupling strategy) and characterization (NMR, IR, elemental analysis, etc.) of a short series of quinoline-oxazole hybrid compounds has been carried out. These materials are found to be moderately active against Plasmodium falciparum in vitro, with activities in the sub-micromolar range, and to display acceptable cytotoxicity to mononuclear leukocytes. Chemical modification strategies, with the intention to increase the biological potency of this new class of anti-malarial agents, are discussed.",

keywords = "Anti-malarial, IC, Oxazoline, Plasmodium falciparum, Pre-clinical evaluation, Toxicity",

author = "Gordey, \{Erin E.\} and Yadav, \{Paras N.\} and Merrin, \{Marcus P.\} and Jill Davies and Steve Ward and Woodman, \{Grant M.J.\} and Sadowy, \{Amber L.\} and Smith, \{Todd G.\} and Gossage, \{Robert A.\}",

year = "2011",

month = aug,

day = "1",

doi = "10.1016/j.bmcl.2011.05.131",

language = "English",

volume = "21",

pages = "4512--4515",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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number = "15",

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Gordey, EE, Yadav, PN, Merrin, MP, Davies, J , Ward, S, Woodman, GMJ, Sadowy, AL, Smith, TG & Gossage, RA 2011, 'Synthesis and biological activities of 4-N-(anilinyl-n-[oxazolyl])-7-chloroquinolines (n=3' or 4') against Plasmodium falciparum in in vitro models.', Bioorganic and Medicinal Chemistry Letters, vol. 21, no. 15, pp. 4512-4515. https://doi.org/10.1016/j.bmcl.2011.05.131

TY - JOUR

T1 - Synthesis and biological activities of 4-N-(anilinyl-n-[oxazolyl])-7-chloroquinolines (n=3' or 4') against Plasmodium falciparum in in vitro models.

AU - Gordey, Erin E.

AU - Yadav, Paras N.

AU - Merrin, Marcus P.

AU - Davies, Jill

AU - Ward, Steve

AU - Woodman, Grant M.J.

AU - Sadowy, Amber L.

AU - Smith, Todd G.

AU - Gossage, Robert A.

PY - 2011/8/1

Y1 - 2011/8/1

N2 - The synthesis (Pd-mediated coupling strategy) and characterization (NMR, IR, elemental analysis, etc.) of a short series of quinoline-oxazole hybrid compounds has been carried out. These materials are found to be moderately active against Plasmodium falciparum in vitro, with activities in the sub-micromolar range, and to display acceptable cytotoxicity to mononuclear leukocytes. Chemical modification strategies, with the intention to increase the biological potency of this new class of anti-malarial agents, are discussed.

AB - The synthesis (Pd-mediated coupling strategy) and characterization (NMR, IR, elemental analysis, etc.) of a short series of quinoline-oxazole hybrid compounds has been carried out. These materials are found to be moderately active against Plasmodium falciparum in vitro, with activities in the sub-micromolar range, and to display acceptable cytotoxicity to mononuclear leukocytes. Chemical modification strategies, with the intention to increase the biological potency of this new class of anti-malarial agents, are discussed.

KW - Anti-malarial

KW - IC

KW - Oxazoline

KW - Plasmodium falciparum

KW - Pre-clinical evaluation

KW - Toxicity

U2 - 10.1016/j.bmcl.2011.05.131

DO - 10.1016/j.bmcl.2011.05.131

M3 - Article

SN - 0960-894X

VL - 21

SP - 4512

EP - 4515

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 15

ER -

Synthesis and biological activities of 4-N-(anilinyl-n-[oxazolyl])-7-chloroquinolines (n=3' or 4') against Plasmodium falciparum in in vitro models.

Abstract

Keywords

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