60912-44-9Relevant academic research and scientific papers
Anti-oligomerization sheet molecules: Design, synthesis and evaluation of inhibitory activities against α-synuclein aggregation
Liu, Hao,Chen, Li,Zhou, Fei,Zhang, Yun-Xiao,Xu, Ji,Xu, Meng,Bai, Su-Ping
supporting information, p. 3089 - 3096 (2019/06/14)
Aggregation of α-synuclein (α-Syn) play a key role in the development of Parkinson Disease (PD). One of the effective approaches is to stabilize the native, monomeric protein with suitable molecule ligands. We have designed and synthesized a series of sheet-like conjugated compounds which possess different skeletons and various heteroatoms in the two blocks located at both ends of linker, which have good π-electron delocalization and high ability of hydrogen-bond formation. They have shown anti-aggregation activities in vitro towards α-Syn with IC50 down to 1.09 μM. The molecule is found binding in parallel to the NACore within NAC domain of α-Syn, interfering aggregation of NAC region within different α-Syn monomer, and further inhibiting or slowing down the formation of α-Syn oligomer nuclei at lag phase. The potential inhibitor obtained by our strategy is considered to be highly efficient to inhibit α-Syn aggregation.
Supramolecular assembly in side-chain conjugated thiophene copolymers
Ananthakrishnan, Soundaram Jeevarathinam,Kumar, Balasubramaniyan Sambath,Somanathan, Narayanasastri,Mandal, Asit Baran
, p. 8331 - 8340 (2013/09/02)
Supramolecular assembly of side chain-conjugated polythiophenes were brought about by a interplay of dipole-dipole interactions and hydrogen bonding. Copolymers of (E)-3,5-dimethyl-4-(2-(thiophene-3-yl)vinyl) isoxazole (DTVI) and (E)-2-(2-(thiophen-3-yl)
From a Multipotent Stilbene to Soluble Epoxide Hydrolase Inhibitors with Antiproliferative Properties
Buscato, Estel.La,Buettner, Dominik,Brueggerhoff, Astrid,Klingler, Franca-Maria,Weber, Julia,Scholz, Bastian,Zivkovic, Aleksandra,Marschalek, Rolf,Stark, Holger,Steinhilber, Dieter,Bode, Helge B.,Proschak, Ewgenij
supporting information, p. 919 - 923 (2013/07/27)
Inspired by nature: Natural product isopropylstilbene was identified as an inhibitor of soluble epoxide hydrolase exhibiting antiproliferative properties. Following the natural product inspired design approach, a library of (E)-styryl-1H-benzo[d]imidazoles was synthesized and evaluated with recombinant enzyme and on several cancer cell lines. Copyright
HETEROCYCLIC MGLU5 ANTAGONISTS
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Page/Page column 60, (2011/04/18)
Compounds (I) (R1 is an optionally substituted C1-C13 heteromonocyclic, heterobicyclic or heterotri cyclic group containing from 1 to 5 heteroatoms selected from N, O and S; R2 is H, an optionally substituted mo
Synthesis and in vitro evaluation of fluorinated styryl benzazoles as amyloid-probes
Ribeiro Morais, Goreti,Vicente Miranda, Hugo,Santos, Isabel C.,Santos, Isabel,Outeiro, Tiago F.,Paulo, Antonio
scheme or table, p. 7698 - 7710 (2012/01/03)
The formation of proteinaceous aggregates is a pathognomonic hallmark of several neurodegenerative disorders such as Alzheimer's and Parkinson's diseases. To date, the final diagnostic for these diseases can only be achieved by immunostaining of post-mortem brain tissues with the commonly used congo red and Thioflavin T/S amyloid-dyes. The interest in developing amyloid-avid radioprobes to be used for protein aggregates imaging by positron emission tomography has grown substantialy, due to the promise in assisting diagnosis of these disorders. To this purpose, the present work describes the synthesis and characterization of four novel fluorinated styryl benzazole derivatives 1-4 by means of the Wittig reaction, as well as their in vitro evaluation as amyloid-probing agents. All compounds were obtained as mixtures of geometric E and Z isomers, with the preferable formation of the E isomer. Photoisomerization reactions allowed for the maximization of the minor Z isomers. The authentic 1-4E/Z isomers were isolated after purification by column chromatography under dark conditions. Profiting from the fluorescence properties of the different geometric isomers of 1-4, their binding affinities towards amyloid fibrils of insulin, α-synuclein and β-amyloid peptide were also measured. These compounds share similarities with Thioflavin T, interacting specifically with fibrillary species with a red-shift in the excitation wavelengths along with an increase in the fluorescence emission intensity. Apparent binding constants were determined and ranged between 1.22 and 23.96 μM-1. The present data suggest that the novel fluorinated styryl benzazole derivatives may prove useful for the design of 18F-labeled amyloid radioprobes.
THERAPEUTIC AGENTS
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Page/Page column 18, (2008/12/08)
The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompas
Toward novel HIV-1 integrase binding inhibitors: Molecular modeling, synthesis, and biological studies
Mugnaini, Claudia,Rajamaki, Suvi,Tintori, Cristina,Corelli, Federico,Massa, Silvio,Witvrouw, Myriam,Debyser, Zeger,Veljkovic, Veljko,Botta, Maurizio
, p. 5370 - 5373 (2008/02/13)
The identification of a novel hit compound as integrase binding inhibitor has been accomplished by means of virtual screening techniques. A small family of structurally related molecules has been synthesized and biologically evaluated with one of the compounds showing an IC50 = 12 μM.
An Efficient Synthesis of 2-Vinylbenzimidazoles from 1-(2-Benzimidazole-2-ylethyl)pyridinium Salts Using an Anion-Exchange Resin
Alcalde, Ermitas,Perez-Garcia, Lluisa,Dinares, Immaculada,Frigola, Jordi
, p. 6516 - 6521 (2007/10/02)
Transformation of several 1-(2-benzimidazol-2-ylethyl)pyridinium salts, obtained by two different procedures, into their corresponding 2-vinylbenzimidazoles either using an anion-exchange resin (OH- form) or in the solid state is described.This approach now allows a facile entry into the almost unknown 2-vinylbenzimidazole monomers.
