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
合成了一系列
氨基亚甲基
双膦酸酯衍
生物,并使用
甲状旁腺激素(
PTH)诱导的大鼠高
钙血症模型(
PIH模型)评估了其抗吸收活性。在这些化合物中,最终选择了(环庚基
氨基)亚甲基双(
膦酸)(3j)进行进一步研究,在
PIH模型和固定化大鼠骨萎缩模型(
DA模型)中证明其效力是
帕米膦酸盐的10倍。讨论了该系列
双膦酸酯的结构-活性关系。