Synthesis and antimalarial activities of some furoxan sulfones and related furazans

Furoxan derivatives bearing a sulfone moiety at position 3 or 4 were synthesized and tested for their antimalarial action on the chloroquine-sensitive D10 and the chloroquine-resistent W2 strains of Plasmodium falciparum. The furazan analogues were considered for comparison. The most active compound...

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Veröffentlicht in:European journal of medicinal chemistry 2005-12, Vol.40 (12), p.1335-1340
Hauptverfasser: Galli, Ubaldina, Lazzarato, Loretta, Bertinaria, Massimo, Sorba, Giovanni, Gasco, Alberto, Parapini, Silvia, Taramelli, Donatella
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container_end_page 1340
container_issue 12
container_start_page 1335
container_title European journal of medicinal chemistry
container_volume 40
creator Galli, Ubaldina
Lazzarato, Loretta
Bertinaria, Massimo
Sorba, Giovanni
Gasco, Alberto
Parapini, Silvia
Taramelli, Donatella
description Furoxan derivatives bearing a sulfone moiety at position 3 or 4 were synthesized and tested for their antimalarial action on the chloroquine-sensitive D10 and the chloroquine-resistent W2 strains of Plasmodium falciparum. The furazan analogues were considered for comparison. The most active compounds were the products in which the –SO 2R groups are at the 3-position of the furoxan system. These latter substances displayed an antimalarial activity in the μM range, possibly related in part to their ability to release NO.
doi_str_mv 10.1016/j.ejmech.2005.05.001
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subjects Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimalarial
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Antiparasitic agents
Biological and medical sciences
Furoxanyl sulfones
Medical sciences
Molecular Structure
Nitric oxide
Oxadiazoles - chemical synthesis
Oxadiazoles - chemistry
Oxadiazoles - pharmacology
Parasitic Sensitivity Tests
Pharmacology. Drug treatments
Plasmodium falciparum
Plasmodium falciparum - drug effects
Structure-Activity Relationship
title Synthesis and antimalarial activities of some furoxan sulfones and related furazans
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