对基架跳跃的分子药物洞察力基于药物发现的成功成功
Ayan Acharya1, Mukul Yadav1, Mithilesh Nagpure1
1National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab 160062, India.
Drug discovery today
|November 28, 2023
概括
创新的脚手架跳跃策略通过创造新的分子空间和改善药物特性来加速药物发现. 本综述强调了药物化学的进步,以实现更快,更成功的药物开发.
科学领域:
- 药用化学 医学化学
- 药物发现 药物发现 药物发现
- 药理学 药理学是指药理学的学科.
背景情况:
- 药物研发需要创新的方法来提高成功率和缩短时间表.
- 跳是药物化学中产生新化学实体的关键策略.
研究的目的:
- 审查药物发现中的创新性脚手架跳跃策略.
- 分析这些策略如何扩大可用药物的分子空间.
- 为了检查由脚手架跳跃导致的药物特性 (药理动力学,生理化学,药理动力学) 的改善.
主要方法:
- 在药物发现中对架跳跃应用的文献评论.
- 对应用在架跳跃化合物中的分子调制的分析.
- 评估产生的药物,临床候选药物和生物活性剂.
主要成果:
- 跨越脚手架的变体已经成功地产生了新的可药物分子空间.
- 许多药物,临床候选药物和临床前候选药物已经从这些策略中出现.
- 分子调制显著增强了药理动力学,生理化学和药理动力学 (P3) 特性.
结论:
- 创新的脚手架跳跃是加速药物发现的强大工具.
- 这一策略有效地创造了具有改进P3特性的新药候选药物.
- 跳在扩大潜在治疗方法的范围方面做出了重大贡献.
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