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Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.
Published: September 2024
AI Article Synopsis
The study explores creating a dual-efficiency agent that functions as both antiresorptive and anabolic treatments for osteoporosis.
Researchers identified various antiosteoporotic chemotypes and established assembly rules leading to the discovery of a promising dual-functional compound.
This compound demonstrates significant abilities to inhibit osteoclastogenesis and stimulate osteoblast differentiation, suggesting its potential as a valuable candidate for osteoporosis drug development.
Article Abstract
Developing a dual-efficiency agent with antiresorptive and anabolic applications is a promising strategy for treating osteoporosis. This study reports the discovery of dual antiosteoporosis agents a chemotype-assembly approach. Chemotype analysis identified 12 antiresorptive and 12 anabolic chemotypes and 7 dual-function chemotype-assembly rules. Based on these assembly rules, a dual-functional compound was discovered. exhibits osteoclastogenesis inhibition with an IC value of 10.28 μM and osteoblast differentiation stimulation at 10 μM. derivatives were designed and synthesized based on the activity relationship of the chemotypes. This yielded a more active compound, , with an osteoclastogenesis inhibition IC value of 0.40 μM and osteoblast differentiation stimulation at 1.0 μM; compound also suppressed bone loss . These results prove that can be a potential lead for antiosteoporosis drug development.
