this study, a series of novel gossypolderivatives were synthesized and screened in vitro for their anti-HIV-1 and anti-H5N1 activities, respectively. Replacing the aldehyde groups of gossypol with some amino acids not only reduced the cytotoxicity but also enhanced the activities against HIV-1 and H5N1. Compounds 13–17 showed more potent activities against HIV-1 and H5N1 than the other gossypol derivatives
在这项研究中,合成了一系列新颖的棉酚衍生物,并在体外对其抗HIV-1和抗H 5 N 1活性进行了筛选。用某些氨基酸取代棉酚的醛基,不仅可以降低细胞毒性,而且还可以增强对HIV-1和H 5 N 1的活性。与其他棉酚衍生物相比,化合物13 – 17对HIV-1和H 5 N 1的活性更强。同时,这些化合物还对H 5 N 1表现出更强的活性。比1-金刚烷胺。棉酚衍生物中缺少COONa基团会导致抗HIV-1活性的丧失,这表明该基团可能在介导抗病毒活性中起重要作用。添加时间分析表明,化合物13 – 17具有与T20相似的抗HIV-1作用机理。分子建模分析表明,化合物13 - 17可能适合的gp41的疏水口袋内通过氢键网络,疏水性接触性强的静电相互作用。
[EN] COMPOSITION CONTAINING ARTESUNATE<br/>[FR] COMPOSITION CONTENANT DE L'ARTÉSUNATE
申请人:ZHAO MING
公开号:WO2017124045A1
公开(公告)日:2017-07-20
The present disclosure provides a composition of artesunate, a process of preparing the same, and a method of treatment.
本公开提供了一种青蒿素的组成,其制备过程以及治疗方法。
A structural investigation of heteroleptic pentavalent antimonials and their leishmanicidal activity
tropica KWH23 parasite, and the cytotoxicity level was also measured on human macrophage blood cells. It was observed that IC50 of the antimonials was 100‐fold superior as compared with the standard antimonial drug used. Cytotoxicity results showed that these antimonials are highly active even at low concentrations and are biocompatible with human macrophages, making them highly promising drug candidates
为了寻找可安全治疗利什曼病等寄生虫病的新药,合成了一系列[SbR 3(OOCR')2 ]型杂合五价锑,并使用元素分析,傅里叶变换红外光谱和多核(1 H和13 C)NMR光谱。羧酸根部分主要是取代的苯甲酸酯,带有一些适合于乙酰或尼古丁配体的配合物。[Sb(p- Tol)3(p- CH 3 C 6 H 4 COO)2 ],[Sb(p- Tol)3(3,5-Cl 2 C 6 H 3 COO)2 ]和[Sb(p- Tol)3(3-nicotinato)2 ]的晶体学测定结果表明,采用的几何形状介于三角锥和方形锥之间,基本上是单体具有五个协调的Sb中心。评估了对热带利什曼原虫KWH23寄生虫的杀利什曼活性,并且还测定了对人巨噬细胞血细胞的细胞毒性水平。观察到IC 50与所使用的标准锑药相比,这种抗生素的使用率高出100倍。细胞毒性结果表明,即使在低浓度下,这些锑也具有很高的活性,并且与人巨噬细胞具有
Water-soluble mesoporphyrin compounds and methods of preparation
申请人:——
公开号:US20040097481A1
公开(公告)日:2004-05-20
Water soluble tin mesoporphyrin compounds are described. Methods of preparation of water soluble metal mesoporphyrin compounds and pharmaceutical preparations are also described.
本文描述了可溶于水的锡中间体卟啉化合物。同时还描述了制备水溶性金属卟啉化合物和制药制剂的方法。
Composition containing artesunate
申请人:Zhao Ming
公开号:US10471042B2
公开(公告)日:2019-11-12
The present disclosure provides a composition of artesunate, a process of preparing the same, and a method of treatment.