Antimalarial activity of 4-(5-trifluoromethyl-1H-pyrazol-1-yl)-chloroquine analogues

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 3, 2006, Pages 649-653

  Cunico, Wilson ^b   Cechinel, Cleber A ^c   Bonacorso, Helio G ^c   Martins, Marcos A P ^c   Zanatta, Nilo ^c   De Souza, Marcus V N ^b   Freitas, Isabela O ^a   Soares, Rodrigo P P ^a   Krettli, Antoniana U ^a  

^a FEDERAL UNIVERSITY OF MINAS GERAIS   (Brazil)

^b INSTITUTO OSWALDO CRUZ   (Brazil)

^c FEDERAL UNIVERSITY OF SANTA MARIA   (Brazil)

Author keywords

4,5 Dihydropyrazole; Antimalarial; Chloroquine analogues

Indexed keywords

ANTIMALARIAL AGENT; HYPOXANTHINE; KETONE DERIVATIVE; PYRAZOLE DERIVATIVE; QUINOLINE DERIVATIVE;

ANIMAL MODEL; ANTIBIOTIC RESISTANCE; ANTIMALARIAL ACTIVITY; ARTICLE; CHEMICAL REACTION KINETICS; CONTROLLED STUDY; MALARIA; MICROBIAL GROWTH; MOUSE; NONHUMAN; PARASITE; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM;

ANIMALS; ANTIMALARIALS; CHLOROQUINE; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MALARIA; PARASITIC SENSITIVITY TESTS; PLASMODIUM FALCIPARUM; PYRAZOLES;

ANIMALIA; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; TRIFLUORO;

EID: 29544446323     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.10.033     Document Type: Article

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28. General procedure for the preparation of 4-(3-substituted-5- trifluoromethyl-5-hydroxy-4,5-dihydro-1H-pyrazol-1-yl)-7-chloroquinolines (2a-h): to a magnetic stirred solution of 1a-h (1 mmol) in MeOH (10 mL), 7-chloro-4-hydrazinoquinoline (1 mmol) was added at room temperature. The mixture was stirred under reflux (64°C) for 15-30 min. The solvent was evaporated under reduced pressure and the solid products 2a-h were recrystallized from a mixture of acetone and water 5:1.
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