特权小分子对抗被忽视的热带疾病:从结构活动关系的角度来看
J Abbasi Shiran1, B Kaboudin2, N Panahi3
1Pharmaceutical Sciences Research Center, Ardabil University of Medical Sciences, Ardabil, PO Code: 5618953141, Iran.
European journal of medicinal chemistry
|April 21, 2024
概括
在全球范围内,被忽视的热带疾病 (NTD) 影响了超过15亿人. 本综述强调了新的抗感染性小分子和打击寄生性NTD药物耐药性的策略.
科学领域:
- 药用化学 医学化学
- 寄生虫学的寄生虫学
- 药物发现 药物发现 药物发现
背景情况:
- 被忽视的热带疾病 (NTDs) 构成了全球重大健康负担,影响超过15亿人.
- 关键的寄生性NTD如莱什曼病,查加斯病 (CD) 和人类非洲试虫病 (HAT) 导致大量的发病率和死亡率,特别是在贫困地区.
- 现有的抗NTD药物面临挑战,包括耐药性,缺乏疫苗,有效性有限,以及不良影响.
研究的目的:
- 审查最近在开发抗感染性小分子对寄生虫NTDs的进展.
- 从结构-活动关系 (SAR) 的角度分析这些代理.
- 探索新兴的扩大抗NTD药物的治疗范围的战略.
主要方法:
- 文献综述,重点关注最近的科学出版物和流行病学报告.
- 分析抗NTD剂的化学结构,特别是,硫和氧基异环.
- 对已识别的化合物的结构-活性关系 (SAR) 数据的检查.
主要成果:
- 许多小分子,通常具有特权的异环基架,已经显示出对寄生虫NTDs的承诺.
- SAR研究对于理解和优化这些抗感染剂的疗效至关重要.
- 新兴的策略旨在克服当前治疗方法的局限性,并扩大治疗选择.
结论:
- 开发具有优化SAR的新型小分子对于解决NTD危机至关重要.
- 对异环化学和创新的治疗策略的持续研究对于有效的NTD控制至关重要.
- 解决药物耐药性和改善药物概况是未来抗NTD药物发现的关键优先事项.
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