Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds

ACS Medicinal Chemistry Letters

Volumn 4, Issue 12, 2013, Pages 1198-1202

  Tukulula, Matshawandile ^a,g   Njoroge, Mathew ^a   Abay, Efrem T ^b,c   Mugumbate, Grace C ^a   Wiesner, Lubbe ^d   Taylor, Dale ^d   Gibhard, Liezl ^d   Norman, Jennifer ^d   Swart, Kenneth J ^c   Gut, Jiri ^e   Rosenthal, Philip J ^e   Barteau, Samuel ^f   Streckfuss, Judith ^f   Kameni Tcheudji, Jacques ^f   Chibale, Kelly ^a  

^a UNIVERSITY OF CAPE TOWN   (South Africa)

^b UNIVERSITY OF THE FREE STATE   (South Africa)

^c PAREXEL INTERNATIONAL   (United States)

^d UNIVERSITY OF CAPE TOWN   (South Africa)

^e UNIVERSITY OF SAN FRANCISCO   (United States)

^f NOVARTIS PHARMA AG   (Switzerland)

^g DSI CSIR Nanotechnology Innovation Centre   (South Africa)

Author keywords

Aminoquinolines; antiplasmodial activity; pharmacokinetics; plasma protein binding

Indexed keywords

4 AMINOQUINOLINE DERIVATIVE; CYTOCHROME P450 2C19; CYTOCHROME P450 2C8; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIMICROBIAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; CHO CELL; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CONFORMATION; DRUG CYTOTOXICITY; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG SCREENING; DRUG SOLUBILITY; DRUG SYNTHESIS; HUMAN; HYDROGEN BOND; IN VITRO STUDY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; METABOLITE; MOUSE; NONHUMAN; PARASITEMIA; PLASMA CLEARANCE; PLASMA PROTEIN BINDING; PLASMODIUM BERGHEI; PLASMODIUM BERGHEI INFECTION; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

EID: 84890540262     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml400311r     Document Type: Article

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