title: Piperazine derivatives of benzimidazole as potential anthelmintics. Part 1: Synthesis and activity of methyl-5-(4-substituted piperazin-1-yl)benzimidazole-2-carbamates.
abstract: A series of 5-(4-substituted piperazin-1-yl)-2-nitroanilines (4) and 5-(4-substituted piperazin-1-yl)benzimidazole-2-carbamates (6) has been synthesized starting from 5-chloro-2-nitroaniline (3) and N-monosubstituted piperazines. Catalytic reduction of 4 with Pd/C followed by treatment with 1,3-dicarbomethoxy-S-methylisothiourea yielded the corresponding methyl-5-(4-substituted piperazin-1-yl)benzimidazole-2-carbamates (6) which were for anthelmintic activity against experimental infections of Trichinella spiralis.
authors.affiliation: Department of Organic Chemistry, University of Santiago de Compostela, Spain.
authors.forename: R M
authors.initials: RM
authors.lastname: Sánchez-Alonso
authors.forename: E
authors.initials: E
authors.lastname: Raviña
authors.forename: L
authors.initials: L
authors.lastname: Santana
authors.forename: G
authors.initials: G
authors.lastname: García-Mera
authors.forename: M
authors.initials: M
authors.lastname: Sanmartín
authors.forename: P
authors.initials: P
authors.lastname: Baltar
mesh_terms: D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D002219:Carbamates / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014234:Trichinella / Q000187:drug effects
chemical_list: D000871:Anthelmintics; D001562:Benzimidazoles; D002219:Carbamates; D010879:Piperazines