High kinetic inertness of a bis-hydrated Gd-complex with a constrained AAZTA-like ligand

Adrienn Vágner; Eliana Gianolio; Silvio Aime; Alessandro Maiocchi; Imre Tóth; Zsolt Baranyai; Lorenzo Tei

doi:10.1039/c6cc04753j

High kinetic inertness of a bis-hydrated Gd-complex with a constrained AAZTA-like ligand

Adrienn Vágner, Eliana Gianolio, Silvio Aime, Alessandro Maiocchi, Imre Tóth, Zsolt Baranyai, Lorenzo Tei

Department of Science and Technological Innovation

Research output: Contribution to journal › Article › peer-review

Abstract

Kinetic inertness is a key property for a Gd-based contrast agent. The Gd^III complex of a cyclohexyl-fused AAZTA derivative shows the highest kinetic inertness for non-macrocyclic bis hydrated (q = 2) Gd^III-complexes with a dissociation half-life of 91 years under physiological conditions, very close to that of macrocyclic clinically approved contrast agents. It also shows optimal relaxometric performance (r₁ = 8.3 mM^-1 s^-1 at 20 MHz and 25 °C) due to the presence of two inner sphere water molecules in fast exchange with bulk water and not displaced by endogenous anions.

Original language	English
Pages (from-to)	11235-11238
Number of pages	4
Journal	Chemical Communications
Volume	52
Issue number	75
DOIs	https://doi.org/10.1039/c6cc04753j
Publication status	Published - 2016

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title = "High kinetic inertness of a bis-hydrated Gd-complex with a constrained AAZTA-like ligand",

abstract = "Kinetic inertness is a key property for a Gd-based contrast agent. The GdIII complex of a cyclohexyl-fused AAZTA derivative shows the highest kinetic inertness for non-macrocyclic bis hydrated (q = 2) GdIII-complexes with a dissociation half-life of 91 years under physiological conditions, very close to that of macrocyclic clinically approved contrast agents. It also shows optimal relaxometric performance (r1 = 8.3 mM-1 s-1 at 20 MHz and 25 °C) due to the presence of two inner sphere water molecules in fast exchange with bulk water and not displaced by endogenous anions.",

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T1 - High kinetic inertness of a bis-hydrated Gd-complex with a constrained AAZTA-like ligand

AU - Vágner, Adrienn

AU - Gianolio, Eliana

AU - Aime, Silvio

AU - Maiocchi, Alessandro

AU - Tóth, Imre

AU - Baranyai, Zsolt

AU - Tei, Lorenzo

PY - 2016

Y1 - 2016

N2 - Kinetic inertness is a key property for a Gd-based contrast agent. The GdIII complex of a cyclohexyl-fused AAZTA derivative shows the highest kinetic inertness for non-macrocyclic bis hydrated (q = 2) GdIII-complexes with a dissociation half-life of 91 years under physiological conditions, very close to that of macrocyclic clinically approved contrast agents. It also shows optimal relaxometric performance (r1 = 8.3 mM-1 s-1 at 20 MHz and 25 °C) due to the presence of two inner sphere water molecules in fast exchange with bulk water and not displaced by endogenous anions.

AB - Kinetic inertness is a key property for a Gd-based contrast agent. The GdIII complex of a cyclohexyl-fused AAZTA derivative shows the highest kinetic inertness for non-macrocyclic bis hydrated (q = 2) GdIII-complexes with a dissociation half-life of 91 years under physiological conditions, very close to that of macrocyclic clinically approved contrast agents. It also shows optimal relaxometric performance (r1 = 8.3 mM-1 s-1 at 20 MHz and 25 °C) due to the presence of two inner sphere water molecules in fast exchange with bulk water and not displaced by endogenous anions.

UR - https://www.scopus.com/pages/publications/84987926219

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DO - 10.1039/c6cc04753j

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VL - 52

SP - 11235

EP - 11238

JO - Chemical Communications

JF - Chemical Communications

IS - 75

ER -

High kinetic inertness of a bis-hydrated Gd-complex with a constrained AAZTA-like ligand

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