15452-38-7Relevant academic research and scientific papers
Benzimidazole, benzoxazole and benzothiazole derivatives as 5HT 2B receptor ligands. Synthesis and preliminary pharmacological evaluation
Giorgioni,Accorroni,Di Stefano,Marucci,Siniscalchi,Claudi
, p. 57 - 73 (2007/10/03)
2-Phenethylbenzimidazole, 2-phenethylbenzoxazole and 2- phenethylbenzothiazole derivatives were synthesized to explore the structural features of the serotonin 5-HT2B receptor antagonists. Those molecules were designed to recognize the 5-HT2B receptor and to discriminate it from the 5-HT2A and 5-HT2c subtypes. All compounds were characterized by binding affinity determination for 5-HT 2A and 5-HT2c subtypes and antagonistic activity for 5-HT2B receptor in rat stomach fundus. None of the new compounds showed affinity for 5-HT2A and 5-HT2c subtypes, but some of them displayed antagonistic activity in rat stomach fundus at micromolar concentrations. Birkhaeuser Boston 2005.
Practicable Syntheses of 2-Hydroxymethyl-substituted Benzimidazoles and 2-Formylbenzimidazole
Ooi, Hong Chin,Suschitzky, Hans
, p. 2871 - 2876 (2007/10/02)
N-Protection of benzimidazole by a diethoxymethyl group, as in , allows exclusive lithiation at the 2-position.This protected anion can be made to react with various electrophiles (e. g. ketones, aldehydes) to yield the corresponding 2-hydroxymethylbenzimidazoles (1).Facile deprotection occurs with acid.Two practicable syntheses of 2-formylbenzimidazole are also described and an indirect route to benzimidazole-2-alcohols is discussed.
