Lead optimization of 3-carboxyl-4(1 H)-quinolones to deliver orally bioavailable antimalarials

Journal of Medicinal Chemistry

Volumn 55, Issue 9, 2012, Pages 4205-4219

  Zhang, Yiqun ^a   Clark, Julie A ^a   Connelly, Michele C ^a   Zhu, Fangyi ^a   Min, Jaeki ^a   Guiguemde, W Armand ^a   Pradhan, Anupam ^b   Iyer, Lalitha ^c   Furimsky, Anna ^c   Gow, Jason ^c   Parman, Toufan ^c   El Mazouni, Farah ^d   Phillips, Margaret A ^d   Kyle, Dennis E ^b   Mirsalis, Jon ^c   Guy, R Kiplin ^a  

^a ST JUDE CHILDREN S RESEARCH HOSPITAL   (United States)

^b UNIVERSITY OF SOUTH FLORIDA   (United States)

^c SRI INTERNATIONAL   (United States)

^d UNIVERSITY OF TEXAS SOUTHWESTERN MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 HEPTYL 7 METHOXY 2 METHYL 4 QUINOLINOL; ANTIMALARIAL AGENT; ATOVAQUONE; CHLOROQUINE; ETHYL 2 (3 CHLOROPHENYL) 6 FLUORO 7 METHOXY 4 OXO 1,4 DIHYDROQUINOLINE 3 CARBOXYLATE; QUINOLONE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTIMALARIAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CELL STRAIN HEK293; CELL STRAIN HEPG2; CYTOTOXICITY TEST; DRUG BIOAVAILABILITY; DRUG CYTOTOXICITY; DRUG DESIGN; DRUG EXPOSURE; DRUG PENETRATION; DRUG POTENCY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ELECTRON TRANSPORT; FEMALE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; MALARIA; MEMBRANE PERMEABILITY; MITOCHONDRION; MOUSE; MULTIDRUG RESISTANCE; NONHUMAN; PARASITE CULTIVATION; PLASMODIUM FALCIPARUM; PROTON NUCLEAR MAGNETIC RESONANCE; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTIMALARIALS; BIOLOGICAL AVAILABILITY; FEMALE; HEP G2 CELLS; HUMANS; MALARIA, FALCIPARUM; MICE; MICE, INBRED ICR; NUCLEAR MAGNETIC RESONANCE, BIOMOLECULAR; PARASITEMIA; PLASMODIUM FALCIPARUM; QUINOLINES; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; SPECTROSCOPY, FOURIER TRANSFORM INFRARED; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84861017466     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm201642z     Document Type: Article

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