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

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.

authors

Takeuchi M,Sakamoto S,Yoshida M,Abe T,Isomura Y

doi

10.1248/cpb.41.688

subject

Has Abstract

pub_date

1993-04-01 00:00:00

pages

688-93

issue

4

eissn

0009-2363

issn

1347-5223

journal_volume

41

pub_type

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