On the search of new I2-IBS aliphatic ligands: bis-guanidino carbonyl derivatives.
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).
Corcoran
Jonathan
J
Centre for Synthesis and Chemical Biology, School of Chemistry, Trinity College Dublin, Dublin 2, Ireland.
Rodriguez
Fernando
F
Rozas
Isabel
I
Meana
J Javier
JJ
Callado
Luis F
LF
D001665:Binding Sites; D019791:Guanidine / Q000737:chemistry*; D008024:Ligands; D008958:Models, Molecular