Galli Ubaldina, Lazzarato Loretta, Bertinaria Massimo, Sorba Giovanni, Gasco Alberto, Parapini Silvia, Taramelli Donatella
Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Università degli Studi del Piemonte Orientale, Via Bovio 6, 28100 Novara, Italy.
Eur J Med Chem. 2005 Dec;40(12):1335-40. doi: 10.1016/j.ejmech.2005.05.001. Epub 2005 Jun 24.
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.
合成了在3位或4位带有砜部分的呋咱衍生物，并测试了它们对氯喹敏感的恶性疟原虫D10株和氯喹耐药的W2株的抗疟作用。考虑了呋咱类似物用于比较。最具活性的化合物是其中-SO2R基团位于呋咱体系3位的产物。这些物质在微摩尔范围内显示出抗疟活性，这可能部分与其释放NO的能力有关。
