103855-01-2Relevant articles and documents
From Cells to Mice to Target: Characterization of NEU-1053 (SB-443342) and Its Analogues for Treatment of Human African Trypanosomiasis
Devine, William G.,Diaz-Gonzalez, Rosario,Ceballos-Perez, Gloria,Rojas, Domingo,Satoh, Takashi,Tear, Westley,Ranade, Ranae M.,Barros-álvarez, Ximena,Hol, Wim G. J.,Buckner, Frederick S.,Navarro, Miguel,Pollastri, Michael P.
, p. 225 - 236 (2017)
Human African trypanosomiasis is a neglected tropical disease that is lethal if left untreated. Existing therapeutics have limited efficacy and severe associated toxicities. 2-(2-(((3-((1H-Benzo[d]imidazol-2-yl)amino)propyl)amino)methyl)-4,6-dichloro-1H-indol-1-yl)ethan-1-ol (NEU-1053) has recently been identified from a high-throughput screen of >42,000 compounds as a highly potent and fast-acting trypanocidal agent capable of curing a bloodstream infection of Trypanosoma brucei in mice. We have designed a library of analogues to probe the structure-activity relationship and improve the predicted central nervous system (CNS) exposure of NEU-1053. We report the activity of these inhibitors of T. brucei, the efficacy of NEU-1053 in a murine CNS model of infection, and identification of the target of NEU-1053 via X-ray crystallography.
INDOLE CARBOXAMIDE DERIVATIVES AND USES THEREOF
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Page/Page column 27, (2014/03/26)
A compound of Formula (I) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the transportation of essential molecules in the mmpL3 pathway: (I) wherein R1, R2, R3, R4, R5 and R6 are as defined herein.
SUBSTITUTED INDOLE COMPOUND
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Page/Page column 182-183, (2010/11/24)
Disclosed is an excellent LXR modulator. A compound represented by the general formula (I): (I) wherein R1, R2, R3 and R4: H, an alkyl which may be substituted, OH, an alkoxy which may be substituted, an amino which may be substituted, a halogeno, a phenyl or the like; R5: H or an alkyl; R6: -COR8 (wherein R8: an alkoxy which may be substituted, a phenyloxy which may be substituted, an amino which may be substituted, or the like), -SO2R9 (wherein R9: an alkyl which may be substituted, a phenyl which may be substituted or a heterocyclyl which may be substituted), or an alkyl which may be substituted; R7: -X2R10 [wherein R10: -COR11 (where R11: OH, an alkoxy which may be substituted or an amino which may be substituted), -SO2R12 (where R12: an alkyl which may be substituted or amino which may be substituted), -N(R13)COR14 (where R13: H or an alkyl which may be substituted; R14: H or an alkyl which may be substituted), -N(R13)SO2R15 (where R13: as defined above; R15: an alkyl which may be substituted) or tetrazol-5-yl; and X2: a single bond or an alkylene which may be substituted]; X1: a methylene which may be substituted; Y1: a phenyl which may be substituted or a heterocyclyl which may be substituted; and Y2: an aryl which may be substituted, a heterocyclyl which may be substituted or the like], or the like.