Structural optimization of quinolon-4(1 H)-imines as dual-stage antimalarials: Toward increased potency and metabolic stability

Journal of Medicinal Chemistry

Volumn 56, Issue 19, 2013, Pages 7679-7690

  Ressurreição, Ana S ^a   Gonçalves, Daniel ^a   Sitoe, Ana R ^a   Albuquerque, Ineîs S ^b   Gut, Jiri ^c   Góis, Ana ^b   Gonçalves, Lídia M ^a   Bronze, Maria R ^a   Hanscheid, Thomas ^b   Biagini, Giancarlo A ^d   Rosenthal, Philip J ^c   Prudeîncio, Miguel ^b   O'Neill, Paul ^e   Mota, Maria M ^b   Lopes, Francisca ^a   Moreira, Rui ^a  

^a RESEARCH INSTITUTE FOR MEDICINES IMED ULISBOA   (Portugal)

^b INSTITUTO DE MEDICINA MOLECULAR   (Portugal)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d LIVERPOOL SCHOOL OF TROPICAL MEDICINE   (United Kingdom)

^e UNIVERSITY OF LIVERPOOL   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMALARIAL AGENT; CHLOROQUINE; GENTAMICIN; MANNICH BASE; QUINOLON 4(1H)IMINE DERIVATIVE; QUINOLONE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANTIMALARIAL ACTIVITY; ARTICLE; CONTROLLED STUDY; CYTOTOXICITY; DRUG POTENCY; DRUG STABILITY; DRUG STRUCTURE; ERYTHROCYTE; HUMAN; HUMAN CELL; IC 50; LIVER MICROSOME; MALARIA FALCIPARUM; MANNICH REACTION; NONHUMAN; PLASMODIUM FALCIPARUM; RAT;

ANIMALS; ANIMALS, GENETICALLY MODIFIED; ANTIMALARIALS; CELL LINE, TUMOR; CRYSTALLIZATION; ELECTRON TRANSPORT COMPLEX III; HEK293 CELLS; HEMEPROTEINS; HUMANS; IMINES; LIFE CYCLE STAGES; MICROSOMES, LIVER; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; QUINOLONES; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84885635225     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm4011466     Document Type: Article

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