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The Synthesis and Evaluation of Quaternary Pyridinium Bisphosphonates as Potent Anti-Resorptives
Authors:G M Blackburn  John Carran  Richard Brown  Joanne Xiong  Donald Watts  Graham Russell
Institution:1. Departments of Chemistry and Molecular Biology , Sheffield University , Sheffield, 53 7HF, UK.;2. Procter &3. Gamble Pharmaceuticals Inc. , Cincinnati, Ohio, USA
Abstract:Abstract

Several novel quaternary pyridinium bisphosphonates have been synthesised and their efficacy as potential anti-resorptive bone agents have been tested in Dictyostelium discoideum. This assay has been shown to accurately reflect the potency of a bisphosphonic acid as an anti-resorptive compound. All the quaternary bisphosphonates are very potent growth inhibitors but results indicate that the more potent compounds are those containing hydrophobic, bulky groups.
Keywords:Bisphosphonate  Anti-resorptive  Dictyostelium  quaternary pyridinium  
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