title: Synthesis and in vitro cysticidal activity of new benzimidazole derivatives.
abstract: 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.
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, México DF 14269, Mexico. ingpalomares@yahoo.com.mx
authors.forename: Francisca
authors.initials: F
authors.lastname: Palomares-Alonso
authors.forename: Helgi
authors.initials: H
authors.lastname: Jung-Cook
authors.forename: Jaime
authors.initials: J
authors.lastname: Pérez-Villanueva
authors.forename: Juan Carlos
authors.initials: JC
authors.lastname: Piliado
authors.forename: Sergio
authors.initials: S
authors.lastname: Rodríguez-Morales
authors.forename: Guadalupe
authors.initials: G
authors.lastname: Palencia-Hernández
authors.forename: Nayeli
authors.initials: N
authors.lastname: López-Balbiaux
authors.forename: Alicia
authors.initials: A
authors.lastname: Hernández-Campos
authors.forename: Rafael
authors.initials: R
authors.lastname: Castillo
authors.forename: Francisco
authors.initials: F
authors.lastname: Hernández-Luis
mesh_terms: D015766:Albendazole / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D008958:Models, Molecular; D012015:Reference Standards; D013621:Taenia / Q000187:drug effects*
chemical_list: D000871:Anthelmintics; D001562:Benzimidazoles; C031000:benzimidazole; D015766:Albendazole; C027186:albendazole sulfoxide