Utilize este identificador para referenciar este registo: http://hdl.handle.net/10400.1/4242
Título: Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates
Autor: Araújo, Nuna C.
Barton, Victoria
Jones, Michael
Stocks, Paul A.
Ward, Stephen A.
Davies, Jill
Bray, Patrick G.
Shone, Alison E.
Cristiano, Maria Lurdes Santos
O'Neill, Paul M.
Palavras-chave: Antimalarial
Resistance
Plasmodium falciparum
Drug-hybrid
Data: 2009
Editora: Elsevier
Citação: Araújo, Nuna C.P.; Barton, Victoria; Jones, Michael; Stocks, Paul A.; Ward, Stephen A.; Davies, Jill; Bray, Patrick G.; Shone, Alison E.; Cristiano, Maria L.S.; O’Neill, Paul M. 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, 19, 7, 2038-2043, 2009.
Resumo: 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.
Peer review: yes
URI: http://hdl.handle.net/10400.1/4242
DOI: http://dx.doi.org/10.1016/j.bmcl.2009.02.013
ISSN: 0960-894X
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