66630-74-8Relevant academic research and scientific papers
Synthesis and antiprotozoal activity of nitazoxanide-N-methylbenzimidazole hybrids
Soria-Arteche, Olivia,Hernandez-Campos, Alicia,Yepez-Mulia, Lilian,Trejo-Soto, Pedro Josue,Hernandez-Luis, Francisco,Gres-Molina, Jorge,Maldonado, Luis A.,Castillo, Rafael
, p. 6838 - 6841 (2014/01/06)
A series of a novel hybrid compounds between nitazoxanide and N-methylbenzimidazole were synthesized starting from the corresponding N-methyl-2-nitroanilines. The new hybrid compounds (1-13) were evaluated in vitro against Giardia intestinalis, Entamoeba
Exploring the interplay of physicochemical properties, membrane permeability and giardicidal activity of some benzimidazole derivatives
Hernández-Covarrubias, Carlos,Vilchis-Reyes, Miguel A.,Yépez-Mulia, Lilian,Sánchez-Díaz, Remedios,Navarrete-Vázquez, Gabriel,Hernández-Campos, Alicia,Castillo, Rafael,Hernández-Luis, Francisco
scheme or table, p. 193 - 204 (2012/07/27)
This study evaluated the relationship between the physicochemical properties, membrane permeability and in vitro giardicidal activity of twenty nine benzimidazole derivatives (1-7n). The retention time data from reverse phase high performance chromatography (RP-HPLC) were used to estimate aqueous solubility and lipophilicity of these compounds. The apparent permeability was determined using Caco-2 cell monolayer. The calculation of some descriptors, such as Clog P, PSA, was performed using ACD labs software. For benzimidazole derivatives with NHCOOCH3, CH3, NH2, SH and SCH3 groups at the 2-position, a quadratic type of regression model was obtained with giardicidal activity and aqueous solubility or lipophilicity. On the other hand, giardicidal activity of 2-(trifluoromethyl)-1H-benzimidazole derivatives was influenced by lipophilicity, hydrogen bond donors and molecular volume but it was not determined by their apparent permeability in Caco-2 cell line.
NOVEL JNK INHIBITORS
-
Page/Page column 105, (2008/12/07)
Disclosed are substituted imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrazines, imidazo[1,2-c]pyrimidines and imidazo[1,2-d]triazines compounds of the formula: (1.0) Also disclosed are methods for treating JNK1 and ERK mediated diseases using the compounds of formula 1.0.
Development of a scalable synthesis of a nonbasic inhibitor of the serine protease tryptase
Dener, Jeffrey M.,O'Bryan, Colin,Yee, Robert,Shelton, Emma J.,Sperandio, David,Mahajan, Tania,Palmer, James T.,Spencer, Jeffrey R.,Tong, Zhiwei
, p. 4591 - 4595 (2007/10/03)
A chromatography-free process for the synthesis of a bis(benzimidazole)difluoromethane inhibitor of the serine protease tryptase is described. This synthesis features the introduction of the gem-difluoro moiety using the electrophilic fluorinating reagent N-fluoro-bis(phenylsulfonimide) as well as the stepwise introduction of both benzimidazole rings. A protocol for the destruction of reactive, process-related substances produced in the synthesis is also presented.
Development summary towards a manufacturable process for R 83842 [(S)-6-[(4-chlorophenyl) (1H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotriazole]
de Knaep,Vandendriessche,Daemen,Dingenen,Laenen,Nijs,Pauwels,van den Heuvel,van der Eycken,Vanierschot,van Laar,Verstappen,Willemsens
, p. 162 - 166 (2013/09/07)
A scalable process to produce enantiomeric R 83842, (S)-6-[(4-chlorophenyl)(1H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotriazole, is developed and described as a lecture * transcript. Cheap and safe reagents have been used. A typical procedure for oxidative destruction of aqueous cyanide waste, and stability data on N-acetyl hydrazine are provided. Special focus is on cost analysis as an important tool in developing performant synthetic methods. The method consists of preparing a chiral monosubstituted hydrazine which is ring closed to the chiral 1-alkylated 1,2,4-triazole title compound.
