RESUMEN
The syntheses of seven anthracene amino alcohols with one, two, or three additional substituents are described. These compounds include three 1-aminoethanols, two 9-aminoethanols, and two 9-aminopropanols, prepared from substituted anthraquinones or from 10-chloro-9-anthraldehydes. The antimalarial activity of these compounds, as well as tentative structure-activity relationships, is discussed in the light of previously published work.
Asunto(s)
Amino Alcoholes , Antracenos , Antimaláricos , Amino Alcoholes/síntesis química , Amino Alcoholes/uso terapéutico , Animales , Antracenos/síntesis química , Antracenos/uso terapéutico , Antimaláricos/síntesis química , Antimaláricos/uso terapéutico , Malaria/tratamiento farmacológico , Ratones , Plasmodium berghei , Relación Estructura-ActividadRESUMEN
A series of substituted 2-pyridyl-alpha-toluenesulfonates was synthesized for antimalarial testing. They were prepared by treating various 2-pyridinols with alpha-toluenesulfonyl chlorides in the presence of an alkali. In tests against Plasmodium berghei in mice at 640 mg/kg, only 3,5-dichloro-2-pyridyl-alpha-toluenesulfonate was considered active, i.e., doubled the mean survival time.