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

Journal Article

TítuloSemi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.
Publication TypeJournal Article
AuthorsAraújo, NCP, Barton, V, Jones, M, Stocks, PA, Ward, SA, Davies, J, Bray, PG, Shone, AE, Cristiano, MLS, O'Neill, PM
Year of Publication2009
JournalBioorg Med Chem Lett
Volume19
Questão7
Date Published2009 Apr 1
Pagination2038-43
ISSN1464-3405
Palavras-chaveAminacrine, Animals, Antimalarials, Artemisinins, Peroxides, Plasmodium falciparum, Quinolines, Structure-Activity Relationship
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.
DOI10.1016/j.bmcl.2009.02.013
Sapientia

http://www.ncbi.nlm.nih.gov/pubmed/19251414?dopt=Abstract
Alternate JournalBioorg. Med. Chem. Lett.
PubMed ID19251414
Grant ListBB/C006321/1 / / Biotechnology and Biological Sciences Research Council / United Kingdom
BBS/B/05508 / / Biotechnology and Biological Sciences Research Council / United Kingdom
BBS/Q/Q/2004/06032 / / Biotechnology and Biological Sciences Research Council / United Kingdom
BBS/S/P/2003/10353 / / Biotechnology and Biological Sciences Research Council / United Kingdom
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