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Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates

Araujo, N. C. P., Barton, V., Jones, M., Stocks, Paul A., Ward, Stephen ORCID: https://orcid.org/0000-0003-2331-3192, Davies, Jill, Bray, Patrick, Shone, Alison, Cristiano, M. L. S. and O'Neill, P. M. (2009) 'Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates'. Bioorganic & Medicinal Chemistry Letters, Vol 19, Issue 7, pp. 2038-2043.

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Abstract

A novel series of semi-synthetic trioxaquines and synthetic trioxolaquines were prepared, in moderate to good yields. Antimalarial activity was evaluated against both the chloroquine-sensitive 3D7 and resistant K1 strain of Plasmodium falciparum and both series of compounds were shown to be active in the low nanomolar range. For comparison the corresponding 9-amino acridine analogues were also prepared and shown to have low nanomolar activity like their quinoline counterparts. (C) 2009 Elsevier Ltd. All rights reserved.

Item Type: Article
Uncontrolled Keywords: antimalarial resistance plasmodium falciparum drug-hybrid parasite-targeted artemisinin mechanism-based design antimalarial activity plasmodium-falciparum derivatives analogs drug dispiro-1,2,4-trioxolanes trioxaquines peroxides
Subjects: WC Communicable Diseases > Tropical and Parasitic Diseases > WC 750 Malaria
QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials
QX Parasitology > Protozoa > QX 135 Plasmodia
QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 254 Antiprotozoal agents (General)
Faculty: Department: Groups (2002 - 2012) > Molecular & Biochemical Parasitology Group
Digital Object Identifer (DOI): https://doi.org/10.1016/j.bmcl.2009.02.013
Depositing User: Mary Creegan
Date Deposited: 22 Jun 2010 09:55
Last Modified: 06 Feb 2018 12:59
URI: https://archive.lstmed.ac.uk/id/eprint/222

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