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

Gordey, Erin E, Yadav, Paras N, Merrin, Marcus P, Davies, Jill, Ward, Stephen ORCID: https://orcid.org/0000-0003-2331-3192, Woodman, Grant M J, Sadowy, Amber L, Smith, Todd G and Gossage, Robert 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 & Medicinal Chemistry Letters, Vol 21, Issue 15, pp. 4512-5.

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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.

Item Type:	Article
Subjects:	QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials QX Parasitology > Protozoa > QX 135 Plasmodia WC Communicable Diseases > Tropical and Parasitic Diseases > WC 750 Malaria
Digital Object Identifer (DOI):	https://doi.org/10.1016/j.bmcl.2011.05.131
Depositing User:	Mary Creegan
Date Deposited:	24 Nov 2011 16:05
Last Modified:	08 Jun 2018 11:12
URI:	https://archive.lstmed.ac.uk/id/eprint/2448

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