Synthesis of 2-pyridyl-alpha-toluenesulfonates as antimalarials.
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.
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D010962:Plasmodium berghei; D013997:Time Factors; D014105:Tosyl Compounds / Q000138:chemical synthesis* / Q000627:therapeutic use
D000962:Antimalarials; D014105:Tosyl Compounds