Benzo[b]thiophen-2-yl(morpholino)methanone and Osteoporosis

In this paper, we applied a chemotype-assembly approach for ligand-based drug discovery (LBDD) to discover novel anti-osteoporosis leads. With this new approach, we identified 12 chemotypes and derived 18 major chemotype assembly rules from 245 known anti-osteoporosis compounds. Then, we selected 19 compounds from an in-house compound library using chemotype-assembly approach for anti-osteoporosis assays, which resulted in 13 hits. Based on structural features in these 13 compounds, we synthesized 50 possible anti-osteoporosis compounds from the anti-osteoporosis chemotypes by means of click chemistry techniques and discovered a compound (10a, IC

Topics: Animals; Bone Density; Bone Resorption; Drug Discovery; Female; Femur; High-Throughput Screening Assays; Ligands; Osteoblasts; Osteoporosis; Rats; Rats, Sprague-Dawley