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-resistant W2 strains of Plasmodium falciparum. The furazan analogues were considered for comparison. The most active compounds were the products in which the -SO2R groups are at the 3-position of the furoxan system. These latter substances displayed an antimalarial activity in the microM range, possibly related in part to their ability to release NO.
Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Università degli Studi del Piemonte Orientale, Via Bovio 6, 28100 Novara, Italy.
Ubaldina
U
Galli
Loretta
L
Lazzarato
Massimo
M
Bertinaria
Giovanni
G
Sorba
Alberto
A
Gasco
Silvia
S
Parapini
Donatella
D
Taramelli
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
D000962:Antimalarials; D010069:Oxadiazoles; C010166:furoxans