Atkinson E R, Granchelli F E
J Pharm Sci. 1976 Apr;65(4):618-20. doi: 10.1002/jps.2600650440.
Four mono- and dialkylated 4-aminobenzothiazoles (VII-X) were prepared as analogs of potent causal prophylactic drugs in the 8-aminoquinoline series. Compounds VII and VIII were toxic at 80 mg/kg in the chick; IX was inactive at 640 mg/kg. In a sporozoite-induced mouse test system, X was inactive at 30 mg/kg and toxic at 480 mg/kg. None of the compounds was active as a suppressive drug.
制备了四种单烷基化和二烷基化的4-氨基苯并噻唑(VII-X)作为8-氨基喹啉系列中强效病因预防药物的类似物。化合物VII和VIII在雏鸡中80mg/kg时具有毒性;化合物IX在640mg/kg时无活性。在子孢子诱导的小鼠试验系统中,化合物X在30mg/kg时无活性,在480mg/kg时具有毒性。这些化合物均无作为抑制性药物的活性。