Studies on Novel Bone Resorption Inhibitors. I. Synthesis and Pharmacological Activites of Aminomethylenebisphosphonate Derivatives.
- 1 January 1993
- journal article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 41 (4) , 688-693
- https://doi.org/10.1248/cpb.41.688
Abstract
A series of aminomethylenebisphosphonate derivatives was synthesized and evaluated for their antiresorptive activities using a parathyroid hormone (PTH)-induced hypercalcemia model in rats (PIH model). Among these compounds, (cycloheptylamino)methylenebis(phosphonic acid) (3j) was finally selected for further investigation, proving 10-fold as potent as pamidronate in the PIH model and an immobilization bone atrophy model in rats (DA model). The structure-activity relationships of this series of bisphosphonates are discussed.Keywords
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