Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: Part 1

Journal of Medicinal Chemistry

Volumn 57, Issue 6, 2014, Pages 2789-2798

  Le Manach, Claire ^a   Gonzàlez Cabrera, Diego ^a   Douelle, Frederic ^a   Nchinda, Aloysius T ^a   Younis, Yassir ^a   Taylor, Dale ^a   Wiesner, Lubbe ^a   White, Karen L ^c   Ryan, Eileen ^c   March, Corinne ^c   Duffy, Sandra ^b   Avery, Vicky M ^b   Waterson, David ^d   Witty, Michael J ^d   Wittlin, Sergio ^e,f   Charman, Susan A ^c   Street, Leslie J ^a   Chibale, Kelly ^a  

^a UNIVERSITY OF CAPE TOWN   (South Africa)

^b GRIFFITH UNIVERSITY   (Australia)

^c MONASH UNIVERSITY   (Australia)

^d ICC   (Switzerland)

^e SWISS TROPICAL AND PUBLIC HEALTH INSTITUTE   (Switzerland)

^f UNIVERSITY OF BASEL   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

6 [3 (METHYLSULFONYL)PHENYL] 3 [4 (METHYLSULFONYL)PHENYL]IMIDAZO[1,2 B]PYRIDAZINE; ANTIMALARIAL AGENT; ARTESUNATE; CHLOROQUINE; IMIDAZOPYRIDAZINE DERIVATIVE; PYRIDAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIMALARIAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CRYSTALLIZATION; DISTRIBUTION VOLUME; DOSE RESPONSE; DRUG ABSORPTION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MICROSOME; MOUSE; NONHUMAN; PARASITEMIA; PHYSICAL CHEMISTRY; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; RAT; SCID MOUSE; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; ANTIMALARIALS; BIOLOGICAL AVAILABILITY; DRUG DESIGN; DRUG RESISTANCE; DRUG STABILITY; GENE LIBRARY; HALF-LIFE; HIGH-THROUGHPUT SCREENING ASSAYS; IMIDAZOLES; MALARIA; MALARIA, FALCIPARUM; MICE; MICE, SCID; PARASITIC SENSITIVITY TESTS; PLASMODIUM; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; PROTEIN KINASE INHIBITORS; PROTEIN KINASES; PYRIDAZINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84897443866     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500098s     Document Type: Article

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