3-阿尔科西-1-基-5-丁醇衍生物是强大的抗莱什曼化合物
Niurka Mollineda-Diogo1, Sergio Sifontes-Rodríguez2, María Magdalena Aguirre-García3
1Centro de Bioactivos Químicos, Universidad Central "Marta Abreu" de Las Villas, Santa Clara, Villa Clara 250512, Cuba.
新的因达衍生物显示出对多种Leishmania物种有前途的抗莱什曼菌活性. 化合物NV6和NV8在前性和前性阶段都表现出有效性,这表明它们可能成为新型抗莱什曼病药物.
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:
- 印达因其抗原动物性质而闻名.
- 莱什曼病仍然是一个重大的全球健康问题,需要新的治疗策略.
研究的目的:
- 评估13种3-基-1-基-5-尼特罗达醇衍生物的体外抗莱什曼性活性.
- 评估这些化合物的细胞毒性和对Leishmania物种的选择性.
主要方法:
- 在体外评估增长抑制活性对促生菌和细胞内促生菌.
- 使用小鼠腹巨细胞的细胞毒性测定.
- 传输和扫描电子显微镜以阐明形态效应.
主要成果:
- 化合物NV6和NV8在生命阶段表现出针对所有三个测试的Leishmania物种 (L. amazonensis,L. infantum,L. mexicana) 的活性.
- 与其他衍生品相比,NV8显示出更高的活性和选择性.
- 3 - 基-1-基-5 - 尼托因达醇衍生物显示出与安福特素B对抗前列腺炎的可比活性.
结论:
- 伊达衍生物,特别是NV6和NV8,在体外具有显著的抗莱什曼病潜力.
- 这些化合物对莱什马尼亚寄生虫的前性和前性形式都表现出有效性.
- 对这种类型的因达尔进行进一步的研究是有必要的,以开发新的抗莱什曼药物.
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
07:30A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones
Published on: January 21, 2020
相关概念视频
Physical Properties of Amines
Preparation of 1° Amines: Azide Synthesis
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Diazonium Group Substitution: –OH and –H
Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions
Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo,...
