RESUMO
Filarial diseases, including lymphatic filariasis and onchocerciasis, are considered among the most devastating of all tropical diseases, affecting about 145 million people worldwide. Efforts to control and eliminate onchocerciasis are impeded by a lack of effective treatments that target the adult filarial stage. Herein, we describe the discovery of a series of substituted di(pyridin-2-yl)-1,2,4-thiadiazol-5-amines as novel macrofilaricides for the treatment of human filarial infections.
Assuntos
Filariose Linfática , Oncocercose , Adulto , Aminas , HumanosRESUMO
[reaction: see text] An asymmetric synthesis of the heavily oxygenated inner sector of amphidinol 3 constituted of C31-C52 is described. The successful pathway highlights construction of the pair of identical tetrahydropyran subunits from a common intermediate.
Assuntos
Alcenos/síntese química , Antifúngicos/síntese química , Dinoflagellida/química , Piranos/síntese química , Aldeídos/química , Alcenos/farmacologia , Animais , Antifúngicos/farmacologia , Compostos de Epóxi/química , Hidrocarbonetos Iodados/química , Modelos Químicos , Oxigênio/química , Piranos/química , Piranos/farmacologia , Estereoisomerismo , Compostos de Vinila/químicaRESUMO
[reaction: see text] The ability of methyl(trifluoromethyl)dioxirane to cleave p-methoxylbenzyl ethers oxidatively in the presence of various additional functional groups has been investigated. These reactions, performed in aqueous acetonitrile, transform a reasonably robust aryl substituent into a dienyl aldehydo ester. The originally generated E,Z-isomer undergoes slow conversion to the more stable E,E-form at 20 degrees C.
RESUMO
A unique photochemical flow reactor featuring quartz tubing, an aluminum mirror and temperature control has been developed for the photo-induced electron-transfer deoxygenation reaction to produce 2'-deoxy and 2',3'-dideoxynucleosides. The continuous flow format significantly increased the efficiency and selectivity of the reaction.