有效地合成了在杂环部分的5位具有丙基,辛基,癸基,十二烷基或十四烷基氨基的几种荧光苯并[ a ]苯恶嗪氯化物。所有化合物的吸收和发射最大值分别在627–638 nm和654–678 nm范围内,并具有良好的荧光量子产率。对它们在乙醇中的光物理性质的研究可以估算酸碱解离常数K a。揭示了随着烷基侧链长度的增加而增强。仅在水性介质中,观察到酸形式与H-聚集体共存。当链长增加时,溶解度显着降低。用于促进苯并[ a ]苯恶嗪鎓染料增溶的残余乙醇(0.2%v / v)可以通过优先溶剂化使碱性形式存在于水溶液中。在存在DNA的情况下进行的光物理研究表明,具有最多8个碳原子的烷基侧链的化合物可以插入DNA核苷酸之间。此外,发现其他形式的DNA结合也是有效的,其中还涉及苯并[ a ]苯恶嗪鎓染料的基本形式。
DOI:
10.1016/j.tet.2009.10.017
作为产物:
描述:
alkaline earth salt of/the/ methylsulfuric acid 生成 N-丙基萘-1-胺
参考文献:
名称:
Bischoff; Mintz, Chemische Berichte, 1892, vol. 25, p. 2324
Efficient copper-catalyzed N-arylations of nitrogen-containing heterocycles and aliphatic amines in water
作者:Xufeng Li、Daoshan Yang、Yuyang Jiang、Hua Fu
DOI:10.1039/c002172e
日期:——
A simple and efficient copper-catalyzed method has been developed for N-arylations of nitrogen-containing heterocycles and aliphatic amines in water. The protocol uses (1E,2E)-oxalaldehyde dioxime (OADO) as the ligand, and water as the solvent, and shows good tolerance towards various functional groups.
N-(Di)icosyl-Substituted Benzo[a]phenoxazinium Chlorides: Synthesis and Evaluation as Near-Infrared Membrane Probes
作者:Sarala Naik、Carla M. A. Alves、Paulo J. G. Coutinho、M. Sameiro T. Gonçalves
DOI:10.1002/ejoc.201001579
日期:2011.5
Five benzo[a]phenoxaziniumchlorides containing alkyl chains with twenty carbon atoms at the 5- or 9-positions of the tetracyclic ring were efficiently synthesised and characterised by UV/Vis and NIR spectroscopy. The absorption and emission maxima in ethanol occur in the range 627-641 nm and 645-676 nm, respectively, with quantum yields varying from 0.14 to 0.38. Preliminary photophysical studies
[EN] COMPOSITIONS COMPRISING TRYPSIN-CLEAVABLE AMPHETAMINE PRODRUGS AND INHIBITORS THEREOF<br/>[FR] COMPOSITIONS COMPRENANT DES PROMÉDICAMENTS DE TYPE AMPHÉTAMINE CLIVABLES PAR TRYPSINE ET LEURS INHIBITEURS
申请人:PHARMACOFORE INC
公开号:WO2011133347A1
公开(公告)日:2011-10-27
Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an amphetamine prodrug that provides enzymatically-controlled release of amphetamine or an amphetamine analog. The composition can further comprise an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of amphetamine or the amphetamine analog from the amphetamine prodrug so as to attenuate enzymatic cleavage of the amphetamine prodrug.
COMPOSITIONS FOR REDUCING RISK OF ADVERSE EVENTS CAUSED BY DRUG-DRUG INTERACTIONS
申请人:JENKINS Thomas E.
公开号:US20120232066A1
公开(公告)日:2012-09-13
The present disclosure provides a composition comprising a GABA
A
agonist and a GI enzyme inhibitor. The present disclosure also provides a composition comprising (a) a GI enzyme inhibitor and (b) a first drug that interacts with a second drug to produce an adverse effect when the second drug is co-ingested as a GI enzyme-cleavable prodrug with the first drug. Such an interaction can be additive or synergistic.
Synthesis and photophysical studies of new benzo[a]phenoxazinium chlorides as potential antifungal agents
作者:M. Inês P.S. Leitão、B. Rama Raju、Sarala Naik、Paulo J.G. Coutinho、Maria João Sousa、M. Sameiro T. Gonçalves
DOI:10.1016/j.tetlet.2016.07.065
日期:2016.8
A set of four new benzo[a]phenoxazinium chlorides possessing ethyl, propyl, decyl and tetradecyl groups at the 9-amino function of the heterocycle along with a propyl group at the 5-amino position was efficiently synthesized. These compounds displayed fluorescence with maximum emission wavelengths of 673 and 685 nm, in anhydrous ethanol and water. All the benzo[a]phenoxazines were evaluated against
有效地合成了一组四个新的苯并[ a ]苯恶嗪氯化物,它们在杂环的9-氨基官能团上具有乙基,丙基,癸基和十四烷基以及在5-氨基位置上具有丙基。这些化合物在无水乙醇和水中显示出最大发射波长为673和685 nm的荧光。在肉汤微量稀释试验中,针对酵母酵母对所有苯并[ a ]吩恶嗪进行了评估。发现它们的抗真菌活性取决于脂族链长度的变化。化合物7的最高MIC活性为1.56μM 包括在杂环核心的9-氨基位置上的二烷基化丙基取代基和在5-氨基位置上的丙基链。