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Molecules 2011, 16(8), 6165-6178; doi:10.3390/molecules16086165
Article

Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents

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Received: 10 June 2011 / Revised: 15 July 2011 / Accepted: 19 July 2011 / Published: 25 July 2011
(This article belongs to the Special Issue Radical Chemistry)
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Abstract

A series of novel zoledronic acid (ZL) derivatives 1-hydroxy-3-(2-methyl-1H-imidazol-1-yl)propane-1,1-diyldiphosphonic acid (MIPrDP), 1-hydroxy-4-(2-methyl-1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (MIBDP), and 1-hydroxy-5-(2-methyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (MIPeDP) were prepared and successfully labeled with 99mTc in high labeling yields. The in vitro stability and in vivo biodistribution of 99mTc-MIPrDP, 99mTc-MIBDP and 99mTc-MIPeDP were investigated and compared. The biodistribution studies indicate that the radiotracer 99mTc-MIPrDP has highly selective uptake in the skeletal system and rapid clearance from soft tissues. The present findings indicate that 99mTc-MIPrDP holds great potential for use in bone imaging.
Keywords: zoledronic acid derivative; 99mTc-labelled diphosphonates; in vitro stability; biodistribution; bone imaging agent zoledronic acid derivative; 99mTc-labelled diphosphonates; in vitro stability; biodistribution; bone imaging agent
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Qiu, L.; Cheng, W.; Lin, J.; Luo, S.; Xue, L.; Pan, J. Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents. Molecules 2011, 16, 6165-6178.

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