Studies on novel bone resorption inhibitors. I. Synthesis and pharmacological activities of aminomethylenebisphosphonate derivatives

DOI: 10.1248/cpb.41.688

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 688 - 693 (1993)

Update date:2022-08-02

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Authors:

Takeuchi

Sakamoto

Yoshida Yoshida

Abe Abe

Isomura Isomura

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Article abstract of DOI:10.1248/cpb.41.688

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.

Full text of DOI:10.1248/cpb.41.688

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