Synthesis of Organic Compounds for Malaria Chemotherapeutic Studies.
Annual progress rept. no. 9, 1 Aug 73-31 Jul 74,
MIDWEST RESEARCH INST KANSAS CITY MO
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Thirty-eight compounds of the following categories have been synthesized, characterized, and submitted for antimalarial evaluation 1 analogs of 2-p-chlorophenyl2-4-piperidyl-tetrahydrofuran 2 quinoline aminoalcohols 3 compounds related to the antimalarial antibiotic furanomycin, and 4 a special 8-aminoquinoline. The following two compounds have shown curative antimalarial activity against P. berghei in the WRAIR screening 1-2,8-bistrifluoromethylquinolyl-1-4-piperidylethanol ethyl ether fumarate, and 2,8-bistrifluoromethyl-alpha-3-piperidyl-4-quinolinemethanol fumarate. 4-1-p-Chlorophenyl-1-ethoxyethyl-1-ethylpiperidine fumarate was found to be against P. berghei at doses of 160-640 mgkg in mice.
- Organic Chemistry