STUDIES ON NOVEL BONE-RESORPTION INHIBITORS .1. SYNTHESIS AND PHARMACOLOGICAL ACTIVITIES OF AMINOMETHYLENEBISPHOSPHONATE DERIVATIVES

Authors
TAKEUCHI M SAKAMOTO S YOSHIDA M ABE T ISOMURA Y
Citation
M. Takeuchi et al., STUDIES ON NOVEL BONE-RESORPTION INHIBITORS .1. SYNTHESIS AND PHARMACOLOGICAL ACTIVITIES OF AMINOMETHYLENEBISPHOSPHONATE DERIVATIVES, Chemical and Pharmaceutical Bulletin, 41(4), 1993, pp. 688-693
Citations number
22
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Chemical and Pharmaceutical Bulletin → ACNP
ISSN journal
00092363
Volume
41
Issue
4
Year of publication
1993
Pages
688 - 693
Database
ISI
SICI code
0009-2363(1993)41:4<688:SONBI.>2.0.ZU;2-W
Abstract
A series of aminomethylenebisphosphonate derivatives was synthesized a nd evaluated for their antiresorptive activities using a parathyroid h ormone (PTH)-induced hypercalcemia model in rats (PIH model). Among th ese compounds, (cycloheptylamino)methylenebis(phosphonic acid) (3j) wa s finally selected for further investigation, proving 10-fold as poten t as pamidronate in the PIH model and an immobilization bone atrophy m odel in rats (DA model). The structure-activity relationships of this series of bisphosphonates are discussed.