Imidazolopiperazines: Hit to lead optimization of new antimalarial agents

Journal of Medicinal Chemistry

Volumn 54, Issue 14, 2011, Pages 5116-5130

  Wu, Tao ^a   Nagle, Advait ^a   Kuhen, Kelli ^a   Gagaring, Kerstin ^a   Borboa, Rachel ^a   Francek, Caroline ^a   Chen, Zhong ^a   Plouffe, David ^a   Goh, Anne ^c   Lakshminarayana, Suresh B ^c   Wu, Jeanette ^c   Ang, Hui Qing ^c   Zeng, Peiting ^c   Kang, Min Low ^c   Tan, William ^c   Tan, Maria ^c   Ye, Nicole ^c   Lin, Xuena ^e   Caldwell, Christopher ^e   Ek, Jared ^a   Skolnik, Suzanne ^e   Liu, Fenghua ^e   Wang, Jianling ^e   Chang, Jonathan ^a   Li, Chun ^a   Hollenbeck, Thomas ^a   Tuntland, Tove ^a   Isbell, John ^a   Fischli, Christoph ^b,d   Brun, Reto ^b,d   Rottmann, Matthias ^b,d   Dartois, Veronique ^c   Keller, Thomas ^c   Diagana, Thierry ^c   Winzeler, Elizabeth ^a   Glynne, Richard ^a   Tully, David C ^a   Chatterjee, Arnab K ^a   more..

^a GENOMICS INSTITUTE OF THE NOVARTIS RESEARCH FOUNDATION   (United States)

^b SWISS TROPICAL AND PUBLIC HEALTH INSTITUTE   (Switzerland)

^c NOVARTIS INSTITUTE FOR TROPICAL DISEASES   (Singapore)

^d UNIVERSITY OF BASEL   (Switzerland)

^e NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (4 FLUOROPHENYL)IMIDAZO[1,2 A]PYRAZIN 3 AMINE; 2 AMINO 1 [2 (2 FLUOROPHENYL) 3 [(4 FLUOROPHENYL)AMINO] 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] 2 METHYLPROPAN 1 ONE; 2 AMINO 1 [2 (3 FLUOROPHENYL) 3 (4 FLUOROPHENYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] 2 METHYLPROPAN 1 ONE; 2 AMINO 1 [2 (3,4 DIFLUOROPHENYL) 3 (PTOLYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] 2 METHYLPROPAN 1 ONE; 2 AMINO 1 [2 (4 CHLOROPHENYL) 3 [(4 FLUOROPHENYL)AMINO] 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL]ETHANONE; 2 AMINO 1 [2 (4 FLUOROPHENYL) 3 (3 FLUOROPHENYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL]ETHANONE; 2 AMINO 1 [2 (4 FLUOROPHENYL) 3 (4 FLUOROPHENYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL) PROPAN 1 ONE; 2 AMINO 1 [2 (4 FLUOROPHENYL) 3 (4 FLUOROPHENYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] 2 METHYLPROPAN 1 ONE; 2 AMINO 1 [2 (4 FLUOROPHENYL) 3 (4 FLUOROPHENYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] 3 METHYLBUTAN 1 ONE; 2 AMINO 1 [2 (4 FLUOROPHENYL) 3 (4 FLUOROPHENYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] 3 PHENYLPROPAN 1 ONE; 2 AMINO 1 [2 (4 FLUOROPHENYL) 3 (4 FLUOROPHENYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL]ETHANONE; 2 AMINO 1 [2 (4 FLUOROPHENYL) 3 (4 FLUOROPHENYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H)YL] 3 PHENYLPROPAN 1 ONE; 2 AMINO 1 [2 (4 FLUOROPHENYL) 3 (4 TOLYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZINE 7(8H) YL] 2 METHYLPROPAN 1 ONE; 2 AMINO 1 [2 (4 FLUOROPHENYL) 3 (PYRIDIN 3 YLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] 2 METHYLPROPAN 1 ONE; 2 AMINO 1 [3 (BENZO[D][1,3]DIOXOL 5 YLAMINO) 2 PHENYL 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] 3 PHENYLPROPAN 1 ONE; 2 AMINO 1 [3 (BENZO[D][1,3]DIOXOL 5 YLAMINO) 2 PHENYL 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] 4 METHYLPENTAN 1 ONE; 2 AMINO 1 [3 (BENZO[D][1,3]DIOXOL 5 YLAMINO) 2 PHENYL 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL]ETHANONE; 2 AMINO 1 [3 (CYCLOHEXYLAMINO) 2 (4 FLUOROPHENYL) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL) 2 METHYLPROPAN 1 ONE; 2 AMINO 1 [3 [(4 FLUOROPHENYL)AMINO) 2 (3 FLUOROPHENYL) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL]ETHANONE; 2 AMINO 1 [3 [(4 FLUOROPHENYL)AMINO] 2 (4 METHOXYPHENYL) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL]ETHANONE; 2 AMINO 1 [3 [(4 FLUOROPHENYL)AMINO] 2 (PTOLYL) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL]ETHANONE; 2 AMINO 1 [3 [(4 FLUOROPHENYL)AMINO] 2 PHENYL 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] 2 METHYLPROPAN 1 ONE; 3 AMINO 1 [2 (4 FLUOROPHENYL) 3 (4 FLUOROPHENYLAMINO) 5,6 DIHYDROIMIDAZO[1,2 A]PYRAZIN 7(8H) YL] PROPAN 1 ONE; ANTIMALARIAL AGENT; IMIDAZOLE DERIVATIVE; IMIDAZOLOPIPERAZINE; MOLECULAR SCAFFOLD; N (TERT BUTYL) 2 (4 FLUOROPHENYL)IMIDAZO[1,2 A]PYRAZIN 3 AMINE; PIPERAZINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIMALARIAL DRUG RESISTANCE; ARTICLE; CELL PROLIFERATION; CONTROLLED STUDY; DRUG DOSE COMPARISON; DRUG EXPOSURE; DRUG POTENCY; DRUG TOLERABILITY; EXPERIMENTAL INFECTION; FEMALE; IN VITRO STUDY; IN VIVO STUDY; MOUSE; NONHUMAN; PARASITEMIA; PHYSICAL CHEMISTRY; PLASMODIUM BERGHEI INFECTION; PLASMODIUM FALCIPARUM; PROCESS OPTIMIZATION; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION; SURVIVAL TIME; WILD TYPE;

AMINO ACIDS; ANILINE COMPOUNDS; ANIMALS; ANTIMALARIALS; BENZENE DERIVATIVES; CELL LINE; DRUG RESISTANCE; FEMALE; HUMANS; IMIDAZOLES; INHIBITORY CONCENTRATION 50; MALARIA; MICE; MICE, INBRED BALB C; PIPERAZINES; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79960645150     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm2003359     Document Type: Article

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