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Gd(III)‐DO3A‐SBMPP: An Effort to Develop the MRI Contrast Agent with Enhanced Relaxivity
Author(s) -
Rangaswamy Sandhya,
Varshney Raunak,
Tiwari Anjani K.,
Sethi Swarndeep K.,
Hemanth kumar B. S.,
Ojha Himanshu,
Mishra Anil K.
Publication year - 2016
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201600814
Subject(s) - gadolinium , chemistry , conjugate , potentiometric titration , ligand (biochemistry) , piperazine , linker , biocompatibility , mri contrast agent , dota , chelation , click chemistry , combinatorial chemistry , ion , organic chemistry , biochemistry , receptor , mathematical analysis , mathematics , computer science , operating system
Rational design of a new class of MR (magnetic resonance) contrast agent for enhance relaxivity has been described. The click chemistry was employed to incorporate two moieties of 1‐(2‐methoxyphenyl)piperazine and serinol as a linker to enhance the affinity at the recognition sites. The designed ligand was attached to DO3A to synthesize DO3A‐serinol‐bis‐MPP (SBMPP) in 89 % yield. Gd‐DO3A‐SBMPP showed enhanced relaxivity r 1 of 10.85±0.04 mM −1 s −1 as compare to known gadolinium based contrast agents in clinics. The potentiometric titration of gadolinium loaded SBMPP exhibited strong selectivity for Gd 3+ over physiological metal ions such as Zn 2+ and Cu 2+ . Thus, the synthesis of bis‐conjugate could be observed as novel, instructive and initial proof of concept for the synthesis of MR contrast agent with enhanced relaxivity. The preliminary findings show the good biocompatibility and potential functionalities of MPP analogue to target brain regions through MRI.