铁介导的还原性循环/氧化用于生成化学多样化的支架:药物发现的方法
Uttam B Karale1, Akash Shinde2, Vikas R Gaikwad2
1Department of Natural Products and Medicinal Chemistry, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, Uttar Pradesh 201 002, India.
Bioorganic chemistry
|July 7, 2023
概括
研究人员从酸中开发了各种化学支架,用于药物发现. 这些支架显示了神经和抗炎应用的前景,特定化合物在临床前模型中显示出显著的潜力.
科学领域:
- 药用化学 医学化学
- 药物发现 药物发现 药物发现
- 合成有机化学 合成有机化学
背景情况:
- 化学多样化的支架是药物发现的关键起点.
- 亚二和亚二二是新型化合物合成的有价值的前体.
研究的目的:
- 开发一个图书馆的各种化学支架从酸/酸.
- 为了评估合成的支架的药物相似性和生物活动.
主要方法:
- 采用一种关键的合成策略,使用铁酸处理,然后在氧气大气下进行反应.
- 合成了十种不同的支架,包括类和类衍生物.
- 进行了体外和体内测试,以评估神经和抗炎活性.
主要成果:
- 成功合成了10个不同的,类似毒品的支架的库.
- 化合物14a和15a表现出显著的神经向性潜力,并促进神经细胞生长.
- 化合物16通过调节NFkB途径并改善败血症状况,表现出强大的抗炎活性.
结论:
- 开发的合成策略为代表性不足的化学多样性提供了机会.
- 已识别的支架具有有前途的神经和抗炎性质.
- 这些发现为产生神经和炎症疾病的新临床前候选人铺平了道路.
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