A Single-Pot Template Reaction Towards a Manganese-Based T1 Contrast Agent

Stasiuk, Graeme J.; Martins, Andre F.; Botta, Mauro; Prior, Timothy J.; Price, Thomas W.; Kenning, Lawrence; Carniato, Fabio; Hoffmann, Sabrina H. L.; Anbu, Sellamuthu

Abstract

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 , and studied the most important physicochemical properties in vitro. MnL displays optimized r relaxivities at both medium (20 and 64 MHz) and high magnetic fields (300 and 400 MHz) and an enhanced r =21.1 mM s (20 MHz, 298 K, pH 7.4) upon binding to BSA (K =4.2×10 M ). In vivo studies show that MnL is cleared intact into the bladder through renal excretion and has a prolonged blood half-life compared to the commercial GdCA Magnevist. MnL shows great promise as a novel MRI contrast agent. Me Me b −1 −1 3 −1 Me Me 1 1 a

Citation

Stasiuk, G. J., Martins, A. F., Botta, M., Prior, T. J., Price, T. W., Kenning, L., Carniato, F., Hoffmann, S. H. L., & Anbu, S. (in press). A Single-Pot Template Reaction Towards a Manganese-Based T1 Contrast Agent. Angewandte Chemie, 60(19), 10736-10744. https://doi.org/10.1002/anie.202100885

• Journal Article Type: Article
• Acceptance Date: Feb 24, 2021
• Online Publication Date: Apr 1, 2021
• Deposit Date: Apr 9, 2021
• Publicly Available Date: Apr 14, 2021
• Journal: Angewandte Chemie - International Edition
• Print ISSN: 1433-7851
• Electronic ISSN: 1521-3773
• Publisher: Wiley
• Peer Reviewed: Peer Reviewed
• Volume: 60
• Issue: 19
• Pages: 10736-10744
• DOI: https://doi.org/10.1002/anie.202100885
• Keywords: Bishydrated MnCA; Blood pool agents; In vivo MRI; Mn-based contrast agents; Template synthesis
• Public URL: https://hull-repository.worktribe.com/output/3747178
• Publisher URL: https://doi.org/10.1002/anie.202100885