氧铁醇N-基碳酸盐结合物作为抗松体和抗莱什曼体剂
Belinda Jimenez-Martin1, Diego A Guerra-Arias2, Antonio Martinez1
1Departamento de Quimica Organica. Facultad de Ciencias, Universidad de Granada, E-18071 Granada, Spain.
新型氧醇合物对Trypanosoma brucei brucei和Leishmania donovani寄生虫表现出强烈的活性. 这些化合物显示出显著的治疗潜力,与原始分子相比,其疗效和选择性得到改善.
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:
- 氧醇是一种天然,具有抗氧化特性.
- 三和莱什曼病是被忽视的热带疾病,治疗选择有限.
- 开发新的抗寄生虫剂对全球健康至关重要.
研究的目的:
- 为了合成新型氧铁醇N-基酸盐合物.
- 评估这些结合物的抗类和抗莱什曼活动.
- 评估合成化合物的细胞毒性与人类细胞系相比.
主要方法:
- 使用化异酸盐合成氧铁醇N-化碳酸盐合物.
- 在体外测试对Trypanosoma brucei brucei和Leishmania donovani (细胞内吸血虫) 的检测.
- 使用人类细胞系 (MRC-5和THP-1) 的细胞毒性评估.
主要成果:
- 五种N-基碳酸衍生物对T. b. brucei (0.20.8μM) 呈现出微小IC50值.
- 对T. b. brucei.观察到活动 (115460倍) 和选择性指数 (47140倍) 的显著增长.
- 五种化合物对L. donovani的IC50值≤10μM,选择性指数高达60倍.
- 带有自由正正二基的化合物比带有受保护基的化合物更活跃.
结论:
- 氧铁醇N-甲基酸盐合物代表了对抗类和抗莱什曼药物开发的有希望的线索.
- 自由的正正二类部分对观察到的抗寄生虫活性很重要.
- 进一步优化可能会导致被忽视的寄生虫疾病的新疗法.
更多相关视频
12:02An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity
Published on: November 2, 2016
10:42Preparation of N-2-alkoxyvinylsulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
相关概念视频
Oxidation of Alkenes: Syn Dihydroxylation with Osmium Tetraoxide
Alkylation of β-Diester Enolates: Malonic Ester Synthesis
Alkynes to Aldehydes and Ketones: Hydroboration-Oxidation
One of the convenient methods for the preparation of aldehydes and ketones is via hydration of alkynes. Hydroboration-oxidation of alkynes is an indirect hydration reaction in which an alkyne is treated with borane followed by oxidation with alkaline peroxide to form an enol that rapidly converts into an aldehyde or a ketone. Terminal alkynes form aldehydes, whereas internal alkynes give ketones as the final product.
Acetals and Thioacetals as Protecting Groups for Aldehydes and Ketones
In the presence of multiple functional groups, when selective reduction of one group over the other is desired, groups like aldehydes and ketones that form acetals...
Phase II Reactions: Sulfation and Conjugation with α-Amino Acids
