College of Chemistry and Chemical Engineering, Zhengzhou Normal University, Zhengzhou, 450044, China.
Department of Orthopedics, China-Japan Union Hospital, Jilin University, Changchun, 130033, China; Department of Orthopedics, The Fourth Affiliated Hospital of Guangxi Medical University/Liu-Zhou Worker's Hospital, Liuzhou, Guangxi, 545005, China.
Eur J Med Chem. 2023 Nov 5;259:115654. doi: 10.1016/j.ejmech.2023.115654. Epub 2023 Jul 16.
Osteoporosis is a metabolic bone disorder typified by a reduction in bone mass and structural degradation of bone tissue, leading to heightened fragility and vulnerability to fractures. The incidence of osteoporosis increases with age, making it a significant public health challenge. The pathogenesis of osteoporosis involves an imbalance between osteoblast-mediated bone formation and resorption. The current treatment options for osteoporosis include bisphosphonates, hormone replacement therapy (HRT), selective estrogen receptor modulators (SERMs), and denosumab. The recent advances in small-molecule drugs for the clinical treatment of osteoporosis offer promising options for improving bone health and reducing fracture risk. This review aims to provide an overview of the clinical applications and synthetic routes of representative small-molecule drugs for the treatment of osteoporosis. A comprehensive understanding of the synthetic methods of drug molecules for osteoporosis may inspire the development of new, more effective, and practical synthetic techniques for treating this condition.
骨质疏松症是一种以骨量减少和骨组织结构退化为特征的代谢性骨病,导致骨骼脆弱易碎,易于骨折。骨质疏松症的发病率随年龄增长而增加,是一个重大的公共卫生挑战。骨质疏松症的发病机制涉及成骨细胞介导的骨形成和吸收之间的失衡。目前治疗骨质疏松症的方法包括双膦酸盐、激素替代疗法(HRT)、选择性雌激素受体调节剂(SERMs)和地舒单抗。最近在用于临床治疗骨质疏松症的小分子药物方面的进展为改善骨骼健康和降低骨折风险提供了有前途的选择。本综述旨在概述治疗骨质疏松症的代表性小分子药物的临床应用和合成途径。全面了解骨质疏松症药物分子的合成方法,可能会启发开发新的、更有效和实用的治疗这种疾病的合成技术。