Design, synthesis, and evaluation of resveratrol derivatives as Aß1–42 aggregation inhibitors, antioxidants, and neuroprotective agents
摘要:
A series of novel resveratrol derivatives were designed, synthesised and evaluated as potential therapeutic agents for the treatment of Alzheimer's disease. Among these compounds, compound 7l, (E)-5-(4-(isopropylamino)styryl)benzene-1,3-diol, exhibited potent beta-amyloid aggregation inhibition activity, which was confirmed by a ThT fluorescence assay (71.65% at 20 mu M) and transmission electron microscopy (TEM). Compound 7l also exhibited good antioxidant activity (4.12 Trolox equivalents in an oxygen radical absorbance capacity assay and a 37% reduction in reactive oxygen species in cells at 10 mu M). The cytotoxicity analysis of compounds 7f, 7i, 7j and 7l indicated that these compounds have lower toxicities than resveratrol at 60 mu M. (C) 2012 Elsevier Ltd. All rights reserved.
Method and apparatus for improving the oxidative thermal stability of distillate fuel
申请人:Taylor Edwin Spencer
公开号:US20050103686A1
公开(公告)日:2005-05-19
The present invention provides methods of improving the thermal oxidative stability of a distillate fuel which comprise selectively reducing the active concentration in the fuel of N—H containing heterocyclic aromatic compounds in which the nitrogen atom of the N—H group is part of the aromatic system, and wherein said fuel also contains an active concentration of metal compounds or will be exposed to active metal compounds in storage or in use. The present invention also provides methods of determining the thermal oxidative stability of a distillate fuel and apparatus for performing said methods.
1,4-disubstituted piperidine derivatives and their use as 11,betahsd1 inhibitors
申请人:Barton John Peter
公开号:US20050256159A1
公开(公告)日:2005-11-17
A method for inhibiting 11βHSD1 by administering a compound of formula (I) is described, wherein A, X, Y, R
1
, R
12
, n, q, and m are as described in the specification. Novel compounds and methods employing them are also described and claimed.
Cyclic Diguanylate G-Quadruplex Inducer-Nitric Oxide Donor Conjugate as a Bifunctional Antibiofilm Agent and Antibacterial Synergist against <i>Pseudomonas aeruginosa</i> with a Hyperbiofilm Phenotype
作者:Qian-Wen Lin、Jin-Qiang Lu、Ye-Si Huang、Jie-Jiao Liu、Wei-Min Chen、Jing Lin
DOI:10.1021/acs.jmedchem.3c00516
日期:2023.9.14
influence the level of cyclicdiguanylate (c-di-GMP), a universal secondary messenger that plays an important role in biofilm formation in bacteria. Based on our previous finding that c-di-GMP G-quadruplex inducers are effective biofilm formation inhibitors, we designed and synthesized a c-di-GMP G-quadruplex inducer-NO donor conjugate (A11@NO) as a bifunctional antibiofilm agent after obtaining the c-di-GMP
Preparation of amino acids from unsaturated hydantoins
申请人:STAUFFER CHEMICAL COMPANY
公开号:EP0177072A2
公开(公告)日:1986-04-09
Amino acids can be easily prepared by reducing unsaturated hydantoins to the corresponding saturated hydantoins by hydrogenating the unsaturated hydantoin using either Raney Nickel catalyst in the presence of more than a stoichiometric amount of caustic or by using zinc and hydrochloric acid followed by hydrolyzing the resultant composition with at least 3 molar equivalents of an alkali metal hydroxide to produce a racemate of an alpha amino acid. The amino acid in suitable derivative form can then be resolved particularly using a two-phase solvent system. The residual isomer of the amino acid remaining after the resolution process can then be racemized using either pyridoxal-5-phosphate or an aliphatic acid in combination with an aldehyde or a ketone. By these procedures, it is possible to obtain high yields of amino acids.
There is disclosed a number of processes for the promotion of the Raney Nickel catalyzed hydrogenation of carbon-carbon double bonds. (a) One process uses tertiary amines to promote the Raney Nickel catalyzed hydrogenation. (b) Another process uses acetylene and acetylene derivatives to promote the Raney Nickel catalyzed hydrogenation. The promotion of Raney Nickel catalyst is particularly suited for the reduction of unsaturated hydantoins to saturated hydantoins and also for the reduction of cyclic and acyclic olefins and diolefins to the corresponding cyclic and acyclic alkanes.