title: On the search of new I2-IBS aliphatic ligands: bis-guanidino carbonyl derivatives.
abstract: Continuing with our search of aliphatic dicationic derivatives as I2-IBS ligands and looking at Amiloride, a known ligand of I2-IBS, we have incorporated the guanidinocarbonyl moiety into our aliphatic compounds with the intention of improving the binding to I2-IBS. Thus, we present the different approaches to the preparation and pharmacological evaluation (in human brain tissue) as I2-IBS ligands of a new series of aliphatic derivatives incorporating the guanidinocarbonyl group and with different chain length (n= 8-12, and 14 methylene groups).
authors.affiliation: Centre for Synthesis and Chemical Biology, School of Chemistry, Trinity College Dublin, Dublin 2, Ireland.
authors.forename: Jonathan
authors.initials: J
authors.lastname: Corcoran
authors.forename: Fernando
authors.initials: F
authors.lastname: Rodriguez
authors.forename: Isabel
authors.initials: I
authors.lastname: Rozas
authors.forename: J Javier
authors.initials: JJ
authors.lastname: Meana
authors.forename: Luis F
authors.initials: LF
authors.lastname: Callado
mesh_terms: D001665:Binding Sites; D019791:Guanidine / Q000737:chemistry*; D008024:Ligands; D008958:Models, Molecular