Synthesis of a DOTA (Gd3+)-conjugate of proton-pump inhibitor pantoprazole for gastric wall imaging studies

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:23

Article

Maharvi, Ghulam M.¹  Bharucha, Adil E.²  Fauq, Abdul H.¹ 

[1] Mayo Clin, Chem Synth Core Facil, Jacksonville, FL 32224 USA

[2] Mayo Clin, Rochester, MN 55905 USA

关键词: Pantoprazole;    Imaging;    Stomach wall;    Contrast agent;    DOTA;    Conjugate;   

DOI  :  10.1016/j.bmcl.2012.06.051

来源: Elsevier

【 摘 要 】

Magnetic resonance imaging (MRI) is used to evaluate gastrointestinal (GI) structure and functions in humans. Despite filling the viscus lumen with a contrast agent, visualization of the viscus wall is limited. To overcome this limitation, we de novo synthesized a conjugate that covalently combines a Gd-based MRI contrast agent, encaged with a chelating agent (DOTA), with pantoprazole, which is a widely used proton pump inhibitor that binds to proton pumps in the stomach and colon. The DOTA linkage was installed at a mechanism-based strategic location in the pantoprazole molecule to minimize a possible negative effect of the structural modification on the drug. It is anticipated that by defining the wall of the stomach and colon, this compound will facilitate functional MRI of the GI tract in humans. (C) 2012 Elsevier Ltd. All rights reserved.

【 授权许可】

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