Search

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 r1 of 10.85±0.04 mM−1s−1 as compare to known gadolinium based contrast agents in clinics. The potentiometric titration of gadolinium loaded SBMPP exhibited strong selectivity for Gd3+ over physiological metal ions such as Zn2+ and Cu2+. 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.