[Synthesis of 4-methyl-5-substituted phenoxy-primaquine analogues and preliminary evaluation on their antimalarial activity]. 1994

B H Zhong, and R X Deng, and Y L Shi, and G F Li, and J X Zhong, and J D Yang, and J Wang
Institute of Microbiology and Epidemiology, Academy of Military Medical Science, Beijing.

On basis of our previous work, seven 4-methyl-5-substituted phenoxy-6-methoxy-8-(1-methyl-4-amino-butylamino)-quinolines (II2-8) were synthesized and their antimalarial activities were preliminarily evaluated. The target compounds were prepared from 2-nitro-4-methoxy-5-bromo-acetanilide as previously described. The structures of II2-8 and all of the unknown intermediates were confirmed by elementary and spectral analyses. Preliminary biological evaluation revealed that all of II2-8 exhibited significant blood schizonticidal activity and were 4-8 times as effective as primaquine in causal prophylactic test in mice.

UI MeSH Term Description Entries
D008288 Malaria A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia. Marsh Fever,Plasmodium Infections,Remittent Fever,Infections, Plasmodium,Paludism,Fever, Marsh,Fever, Remittent,Infection, Plasmodium,Plasmodium Infection
D010962 Plasmodium berghei A protozoan parasite of rodents transmitted by the mosquito Anopheles dureni. Plasmodium bergheus,berghei, Plasmodium
D011319 Primaquine An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404) Primacin,Primaquine Diphosphate,Primaquine Phosphate,Diphosphate, Primaquine,Phosphate, Primaquine
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000962 Antimalarials Agents used in the treatment of malaria. They are usually classified on the basis of their action against plasmodia at different stages in their life cycle in the human. (From AMA, Drug Evaluations Annual, 1992, p1585) Anti-Malarial,Antimalarial,Antimalarial Agent,Antimalarial Drug,Anti-Malarials,Antimalarial Agents,Antimalarial Drugs,Agent, Antimalarial,Agents, Antimalarial,Anti Malarial,Anti Malarials,Drug, Antimalarial,Drugs, Antimalarial
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus

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