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

• 竹内 誠

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 坂本 修一

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 吉田 誠

  Patent Department, Yamanouchi Pharmaceutical Co., Ltd.

• 阿部 哲士

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 磯村 八州男

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

抄録

A series of aminomethylenebisphosphonate derivatives was synthesized and evaluated for their antiresorptive activities using a parathyroid hormone (PTH)-induced hypercalemia 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.

収録刊行物

• Chem Pharm Bull (Tokyo)

  Chem Pharm Bull (Tokyo) 41 688-693, 1993

  公益社団法人日本薬学会

キーワード

• bisphosphonate
• YM175
• bone resorption inhibitor
• osteoporosis
• pamidronate
• etidronate

詳細情報

• CRID: 1573387452161176960
• NII論文ID: 110003630475
• NII書誌ID: AA00602100
• ISSN: 00092363
• Web Site: https://search.jamas.or.jp/link/ui/1995082302
• 本文言語コード: en
• データソース種別:
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