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

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

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)2808-2811
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number9
DOIs
StatePublished - May 1 2013

Keywords

  • Conjugate
  • Contrast agent
  • DOTA
  • Imaging
  • Pantoprazole
  • Stomach wall

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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