16728-68-0Relevant academic research and scientific papers
Synthesis, biological evaluation of 9-N-substituted berberine derivatives as multi-functional agents of antioxidant, inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation
Shan, Wen-Jun,Huang, Ling,Zhou, Qi,Meng, Fan-Chao,Li, Xing-Shu
, p. 5885 - 5893 (2012/01/04)
A series of 9-N-substituted berberine derivatives were synthesized and biologically evaluated as antioxidant and inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase and amyloid-β aggregation. Most of these compounds exhibited very good antioxidant activities, inhibitive activities of AChE and amyloid-β aggregation. Among them, compound 8d, (o-methylphenethyl)amino linked at the 9-position of berberine, was found to be a good antioxidant (with 4.05 μM of Trolox equivalents), potent inhibitor of AChE (an IC50 value of 0.027 μM), and high active inhibitor of amyloid-β aggregation (an IC50 value of 2.73 μM).
End-quenching of TiCl4-catalyzed quasiliving polyisobutylene with alkoxybenzenes for direct chain end functionalization
Morgan, David L.,Martinez-Castro, Nemesio,Storey, Robson F.
, p. 8724 - 8740 (2011/12/02)
Alkoxybenzenes were used to end-quench TiCl4-catalyzed quasiliving isobutylene polymerizations initiated from 2-chloro-2,2,4- trimethylpentane or 5-tert-butyl-1,3-di(1-chloro-1-methylethyl)benzene at -70 °C in 40/60 (v/v) hexane/methyl chloride. The alkoxybenzene/chain end molar ratios were in the range 2.5-4. Effective alkoxybenzene quenchers included those with simple alkyl groups, such as anisole and isopropoxybenzene, haloalkyl tethers, such as (3-bromopropoxy)benzene and (2-chloroethoxy)benzene, and even those with hydroxyl and amine functionality, such as 4-phenoxy-1-butanol and 6-phenoxyhexylamine. Alkylation was generally quantitative and occurred exclusively in the para position; multiple alkylations on the same alkoxybenzene were not observed. The alkylation reactions were tolerant of temperatures ranging from -70 to -30 °C and were unimpeded by the presence of endo- or exo-olefin termini. In situ cleavage of the ether linkage of anisole and isopropoxybenzene termini allowed single pot syntheses of phenol-terminated polyisobutylenes.
Derivatives of squaric acid with anti-proliferative activity
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Page/Page column 25, (2008/12/08)
The present invention provides derivatives of squaric acid, in particular derivatives of 3,4-diamino-cyclobut-3-ene-1,2-dione and tautomers and isomers thereof, as a single stereoisomer or a mixture of stereoisomers, or as a pharmaceutically acceptable sa
Derivatives of squaric acid with anti-proliferative activity
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Page/Page column 35, (2008/06/13)
The present invention provides derivatives of squaric acid, in particular derivatives of 3,4-diamino-cyclobut-3-ene-1,2-dione and tautomers thereof, as a single stereoisomer or a mixture of stereoisomers, or as a pharmaceutically acceptable salt thereof.
Self-assembly and dynamics of [2]- and [3]rotaxanes with a dinuclear macrocycle containing reversible Os-N coordinate bonds
Chang, Sung-Youn,Choi, Jeung Soon,Jeong, Kyu-Sung
, p. 2687 - 2697 (2007/10/03)
With a dinuclear macrocycle 2 that contains weak reversible OsVI-N coordinate bonds, self-assembly and equilibrium dynamics of [2]- and [3]rotaxanes have been investigated. When the macrocycle 2 was mixed together with threads 4a-e, which all contain an adipamide station but different sizes of end groups, [2]pseudorotaxane- and rotaxane-like complexes were immediately formed with large association constants > of 7 × 103M-1 in CDCl3 at 298 K. Exchange dynamics, explored by 2D-EXSY experiments, suggest that assembly and disassembly of complexes occur through two distinct pathways, slipping or clipping, and this depends on the size of the end groups. The slipping pathway is predominant with smaller end groups that give pseudorotaxane-like complexes, while the clipping pathway is observed with larger end groups that yield rotaxane-like complexes. Under the same conditions, exchange barriers (ΔG≠) were 14.3 kcal mol-1 for 4a and 16.7 kcal mol-1 for 4d, and indicate that the slipping process is at least one order of magnitude faster than the clipping process. Using threads 13a and 13b that contain two adipamide groups, more complicated systems have been investigated in which [2]rotaxane, [3]rotaxane, and free components are in equilibrium. Concentration- and temperature-dependent 1H NMR spectroscopic studies allowed the identification of all possible elements and the determination of their relative distributions in solution. For example, the relative distribution of the free components, [2]rotaxane, and [3]rotaxane are 30, 45, and 25%, respectively, in a mixture of 2 (2mM) and 13a (2mM) in CDCl3, at 10°C. However, [3]rotaxane exists nearly quantitatively in a mixture of 2 (4mM) and 13a (2mM) in CDCl3 at a low temperature - 10°C.
