Improved Inhibitors of Trypanothione Reductase by Combination of Motifs: Synthesis, Inhibitory Potency, Binding Mode, and Antiprotozoal Activities

ChemMedChem

Volumn 6, Issue 2, 2011, Pages 292-301

  Eberle, Christian ^a   Lauber, Birgit Sophia ^a   Fankhauser, Daniel ^a   Kaiser, Marcel ^b,c   Brun, Reto ^b,c   Krauth Siegel, R Luise ^d   Diederich, François ^a  

^a ETH ZURICH   (Switzerland)

^b SWISS TROPICAL AND PUBLIC HEALTH INSTITUTE   (Switzerland)

^c UNIVERSITY OF BASEL   (Switzerland)

^d UNIVERSITY OF HEIDELBERG   (Germany)

Author keywords

Antimalarial agents; Structure based design; Tropical diseases; Trypanocidal agents; Trypanothione reductases

Indexed keywords

1 [1 (BENZO[B]THIOPHEN 2 YL)CYCLOHEXYL] 4 [[1 [2,6 BIS(PHENYLTHIO)PHENYL) 1H 1,2,3 TRIAZOL 4 YL]METHYL]PIPERAZINE; 1 [2 [2,6 BIS(PHENYLTHIO)PHENYL] 1H IMIDAZOL 5 YL] N (3,4 DICHLOROBENZYL) N,N DIMETHYLMETHANAMINIUM FORMATE; 1 [2 [2,6 BIS(PHENYLTHIO)PHENYL] 1H IMIDAZOL 5 YL] N [[2 [2,6 BIS(PHENYLTHIO)PHENYL] 1H IMIDAZOL 5 YL]METHYL] N,N DIMETHYLMETHANAMINIUM FORMATE; 1 [[2 [2,6 BIS(PHENYLTHIO)PHENYL] 1H IMIDAZOL 5 YL]METHYL] 4 METHYLPIPERAZINE; ANTIPROTOZOAL AGENT; GLUTATHIONE REDUCTASE; IMIDAZOLE DERIVATIVE; SULFIDE; TRYPANOTHIONE REDUCTASE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANTIPROTOZOAL ACTIVITY; ARTICLE; BINDING AFFINITY; COMPUTER MODEL; CONTROLLED STUDY; DRUG BINDING; DRUG CYTOTOXICITY; DRUG DESIGN; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME BINDING; ENZYME INHIBITION; IC 50; IN VITRO STUDY; LEISHMANIA DONOVANI; MOLECULAR MODEL; NONHUMAN; PLASMODIUM FALCIPARUM; PREDICTION; PRIORITY JOURNAL; RAT; TRYPANOSOMA CRUZI; TRYPANOSOMA RHODESIENSE;

AMINO ACID MOTIFS; ANTIPROTOZOAL AGENTS; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; MODELS, MOLECULAR; NADH, NADPH OXIDOREDUCTASES;

EID: 79251537792     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201000420     Document Type: Article

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