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