Flavones as isosteres of 4(1H)-quinolones: Discovery of ligand efficient and dual stage antimalarial lead compounds

European Journal of Medicinal Chemistry

Volumn 69, Issue , 2013, Pages 872-880

  Rodrigues, Tiago ^a,e   Ressurreição, Ana S ^a   Da Cruz, Filipa P ^b   Albuquerque, Inês S ^b   Gut, Jiri ^c   Carrasco, Marta P ^a   Gonçalves, Daniel ^a   Guedes, Rita C ^a   Dos Santos, Daniel J V A ^a,d   Mota, Maria M ^b   Rosenthal, Philip J ^c   Moreira, Rui ^a   Prudêncio, Miguel ^b   Lopes, Francisca ^a  

^a RESEARCH INSTITUTE FOR MEDICINES IMED ULISBOA   (Portugal)

^b INSTITUTO DE MEDICINA MOLECULAR   (Portugal)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d UNIVERSITY OF PORTO   (Portugal)

^e ETH ZURICH   (Switzerland)

Author keywords

Dual stage inhibitor; Flavone; Ligand efficiency; Malaria

Indexed keywords

2 [(1,1 BIPHENYL) 4 YL] 6 CHLORO 7 METHYL 4H CHROMEN 4 ONE; 2 [(1,1' BIPHENYL) 4 YL] 3 BROMO 6 CHLORO 7 METHYL 4H CHROMEN 4 ONE; 2 [(1,1' BIPHENYL) 4 YL] 3 BROMO 7 BROMOMETHYL 6 CHLORO 4H CHROMEN 4 ONE; 2 [(1,1' BIPHENYL) 4 YL] 4H CHROMEN 4 ONE; 2 [4 (4 CHLOROPHENOXY)PHENYL] 4H CHROMEN 4 ONE; 2 [4 (4 CHLOROPHENOXY)PHENYL] 7 METHYL 4H CHROMEN 4 ONE; 2 [4 (6 AMINOPYRIDIN 3 YL)PHENYL] 4H CHROMEN 4 ONE; 2 [4 (QUINOLIN 3 YL)PHENYL] 4H CHROMEN 4 ONE; 2 [4 [3 (TRIFLUOROMETHOXY)PHENOXY]PHENYL] 4H CHROMEN 4 ONE; 2 [4' CHLORO (1,1' BIPHENYL) 4 YL] 4H CHROMEN 4 ONE; 2 [4' FLUORO (1,1' BIPHENYL) 4 YL] 4H CHROMEN 4 ONE; 3 (4 BROMOPHENYL) 4H CHROMEN 4 ONE; 4' (4 OXO 4H CHROMEN 2 YL)(1,1' BIPHENYL) 4 CARBALDEHYDE; 6 CHLORO 2 [4 (4 CHLOROPHENOXY)PHENYL] 4H CHROMEN 4 ONE; 6 CHLORO 7 METHYL 2 [4 (4,4,4 TRIFLUOROBUTOXY)PHENYL] 4H CHROMEN 4 ONE; 7 CHLORO 2 [4 (4 CHLOROPHENOXY)PHENYL] 4H CHROMEN 4 ONE; ANTIMALARIAL AGENT; FLAVONE DERIVATIVE; GENISTEIN; UNCLASSIFIED DRUG;

ANTIMALARIAL ACTIVITY; ANTIMALARIAL DRUG RESISTANCE; ARTICLE; CONTROLLED STUDY; DRUG POTENCY; DRUG SYNTHESIS; IC 50; IN VITRO STUDY; MALARIA FALCIPARUM; NONHUMAN; PHYSICAL CHEMISTRY; PLASMODIUM BERGHEI INFECTION; STRUCTURE ACTIVITY RELATION;

1,8-DIAZABICYCLOUNDEC-7-ENE; CHLOROQUINE; CQ; DBU; DMF; DUAL STAGE INHIBITOR; EEF; EXO-ERYTHROCYTIC FORM; FLAVONE; LE; LIGAND EFFICIENCY; MALARIA; N,N-DIMETHYLFORMAMIDE; N-BROMOSUCCINIMIDE; NBS; PFNDH2; PLASMODIUM FALCIPARUM NADH:UBIQUINONE OXIDOREDUCTASE; SAR; STRUCTURE-ACTIVITY RELATIONSHIPS;

ANTIMALARIALS; DOSE-RESPONSE RELATIONSHIP, DRUG; FLAVONES; LIGANDS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PARASITIC SENSITIVITY TESTS; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; QUINOLONES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84885342864     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2013.09.008     Document Type: Article

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