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A Single‐Pot Template Reaction Towards a Manganese‐Based T 1 Contrast Agent
Author(s) -
Anbu Sellamuthu,
Hoffmann Sabrina H. L.,
Carniato Fabio,
Kenning Lawrence,
Price Thomas W.,
Prior Timothy J.,
Botta Mauro,
Martins Andre F.,
Stasiuk Graeme J.
Publication year - 2021
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.202100885
Subject(s) - gadolinium , in vivo , manganese , chemistry , clearance , contrast (vision) , lability , chelation , mri contrast agent , combinatorial chemistry , nuclear magnetic resonance , inorganic chemistry , organic chemistry , computer science , medicine , physics , microbiology and biotechnology , artificial intelligence , urology , biology
Manganese‐based contrast agents (MnCAs) have emerged as suitable alternatives to gadolinium‐based contrast agents (GdCAs). However, due to their kinetic lability and laborious synthetic procedures, only a few MnCAs have found clinical MRI application. In this work, we have employed a highly innovative single‐pot template synthetic strategy to develop a MnCA, MnL Me , and studied the most important physicochemical properties in vitro. MnL Me displays optimized r 1 relaxivities at both medium (20 and 64 MHz) and high magnetic fields (300 and 400 MHz) and an enhanced r 1 b =21.1 mM −1 s −1 (20 MHz, 298 K, pH 7.4) upon binding to BSA ( K a =4.2×10 3 M −1 ). In vivo studies show that MnL Me is cleared intact into the bladder through renal excretion and has a prolonged blood half‐life compared to the commercial GdCA Magnevist. MnL Me shows great promise as a novel MRI contrast agent.