20367-38-8Relevant academic research and scientific papers
SPECIFIC INHIBITORS OF METHIONYL-TRNA SYNTHETASE
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Paragraph 0336, (2016/03/13)
The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.
Synthesis and in vitro cysticidal activity of new benzimidazole derivatives
Palomares-Alonso, Francisca,Jung-Cook, Helgi,Perez-Villanueva, Jaime,Piliado, Juan Carlos,Rodriguez-Morales, Sergio,Palencia-Hernandez, Guadalupe,Lopez-Balbiaux, Nayeli,Hernandez-Campos, Alicia,Castillo, Rafael,Hernandez-Luis, Francisco
body text, p. 1794 - 1800 (2009/07/18)
Despite albendazole being the drug of choice in neurocysticercosis treatment, its low solubility limits its bioavailability; therefore, more research is required in order to find new molecules with cestocidal activity and adequate aqueous solubility. A set of 13 benzimidazole derivatives were synthesized and their in vitro activities were evaluated against Taenia crassiceps cysts, using albendazole sulfoxide as reference molecule, showing that two of them exhibited good activity. Molecular modelling revealed that the cysticidal efficacy depends on the presence on the molecule of an H in the 1-position, a planar carbamate group at 2-position, and if the substituent in 5-position is voluminous, it should be orthogonal to the benzimidazole ring.
Synthesis and antiparasitic activity of 1H-benzimidazole derivatives.
Valdez, Juan,Cedillo, Roberto,Hernandez-Campos, Alicia,Yepez, Lilian,Hernandez-Luis, Francisco,Navarrete-Vazquez, Gabriel,Tapia, Amparo,Cortes, Rafael,Hernandez, Manuel,Castillo, Rafael
, p. 2221 - 2224 (2007/10/03)
Compounds 1-18 have been synthesized and tested in vitro against the protozoa Giardia lamblia, Entamoeba histolytica and the helminth Trichinella spiralis. Inhibition of rat brain tubulin polymerization was also measured and compared for each compound. Results indicate that most of the compounds tested were more active as antiprotozoal agents than Metronidazole and Albendazole. None of the compounds was as active as Albendazole against T. spiralis. Although only compounds 3, 9 and 15 (2-methoxycarbonylamino derivatives) inhibited tubulin polymerization, these were not the most potent antiparasitic compounds.
N-Phenyl-N'-cyano-O-phenylisoureas
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, (2008/06/13)
N-Phenyl-N'-cyano-O-phenylisoureas are prepared from N-cyanodiphenoxyimidocarbonate and an optionally substituted o-phenylenediamine or o-aminophenol. The isoureas are new chemical intermediates especially useful for preparing 2-cyanamido and 2-carbometho
