筛选了基于s-三嗪的杂种的面向多样性的文库,以研究其对氯喹抗性恶性疟原虫W2菌株的活性。最惊人的结果是对含有一个或两个8-氨基喹啉部分的杂合分子的培养的红细胞阶段寄生虫具有亚微摩尔活性。这些化合物对人体细胞没有明显的毒性。然后筛选出最有效的血液杀schizontosdal s -triazine衍生物对抗疟原虫肝阶段的活性。所述š含有两个8-氨基喹啉结构部分和一个氯原子成为最有力的抵抗嗪混合伯氏疟原虫肝阶段感染,在低纳摩尔区域活跃,并在大鼠肝微粒体中具有良好的代谢稳定性。这些结果表明,基于s-三嗪-8-氨基喹啉的杂种作为双阶段抗疟药是铅优化的极佳起点。
Preparation of Antibodies and Development of an Enzyme-Linked Immunosorbent Assay for Determination of Dealkylated Hydroxytriazines
作者:Nuria Sanvicens、Valerie Pichon、Marie-Claire Hennion、M.-Pilar Marco
DOI:10.1021/jf025640v
日期:2003.1.1
The development of an indirect competitive enzyme-linked immunosorbent assay (ELISA) for dealkylated hydroxytriazines is reported here for the first time. The assay uses polyclonal antibodies raised against N-(4-amine-6-hydroxy-[1,3,5]triazin-2-yl)-4-aminobutanoic acid (hapten 2g) conjugated to keyhole limpet hemocyanin by the active ester method. The immunizing hapten was synthesized by first introducing the amino group to the triazine ring in a protected form in order to increase its solubility in organic media. Subsequent steps consisted of reacting this compound with an appropriate spacer arm, followed by removal of the protecting group in acidic media. The resulting assay uses a homologous competitor hapten coupled to conalbumin by the mixed anhydride method. Coating antigens prepared using a homologous covalent coupling procedure failed to produce competitive immunoassays. The assay tolerates media with high ionic strength (up to 70 mS cm(-1)) and basic pH values (7.5-9.5 units). Under the optimized conditions, this ELISA is specific. for dealkylated hydroxytriazines, reaching suitable limits of detection.
[EN] THIOREDOXIN MODULATORS AND USES THEREOF<br/>[FR] MODULATEURS DE THIORÉDOXINE ET LEURS UTILISATIONS
申请人:UNIV CALIFORNIA
公开号:WO2018175958A1
公开(公告)日:2018-09-27
Described herein, inter alia, are compounds and methods for modulating thioredoxin.