Synthesis of novel bone-targeted agents for treatment of osteoporosis

Novel bone-targeted agents have been designed and synthesized by the combination of raloxifene and bisphosphonates. The anti-osteoporosis effect has been evaluated by bone mineral density (BMD) obtained from ovariectomized (OVX) mice in vivo. The results indicate that the compounds 8 and 9 not only prevent ovariectomy induced loss of bone but also enhance BMD to 7.09 and 12.59% compared to sham-operated control, respectively.