A robust and convergent synthesis of dipeptide-DOTAM conjugates as chelators for lanthanide ions: new PARACEST MRI agents |
| |
Authors: | Wojciechowski Filip Suchy Mojmir Li Alex X Azab Hassan A Bartha Robert Hudson Robert H E |
| |
Institution: | Department of Chemistry, The University of Western Ontario, London, Ontario, Canada N6A 5B7. |
| |
Abstract: | A generally applicable synthetic approach to dipeptide-DOTAM conjugates has been developed which is based on the peralkylation of 1,4,7,10-tetraazacyclododecane (cyclen) with protected N-iodoacetyl dipeptides. Standardized procedures were used for the alkylation, metalation, and purification of the resultant lanthanide complexes. Using this approach, we have been able to rapidly and reliably prepare and screen five different ligands each with up to six lanthanide ions. This preliminary investigation has identified several paramagnetic compounds with strong chemical exchange saturation transfer (PARACEST) properties in water at physiological temperature and pH. Extension of the synthetic approach to a wide variety of amino acids is possible. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|