65591-91-5Relevant academic research and scientific papers
Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors
Suzuki, Sayaka,Kuroda, Takeshi,Kimoto, Hiroko,Domon, Yuki,Kubota, Kazufumi,Kitano, Yutaka,Yokoyama, Tomihisa,Shimizugawa, Akiko,Sugita, Ryusuke,Koishi, Ryuta,Asano, Daigo,Tamaki, Kazuhiko,Shinozuka, Tsuyoshi,Kobayashi, Hiroyuki
, p. 5419 - 5423 (2015)
A novel class of NaV1.7 inhibitors has been identified by high-throughput screening followed by structure activity relationship studies. Among this series of compounds, piperidine 9o showed potent human and mouse NaV1.7 inhibitory activities with fair subtype selectivity over NaV1.5. Compound 9o successfully demonstrated analgesic efficacy in mice comparable to that of the currently used drug, mexiletine, but with an expanded central nervous system safety margin.
NOVEL POLYMERIC PHOTOINITIATORS AND PHOTOINITIATOR MONOMERS
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Page/Page column, (2015/06/03)
The present invention provides polymeric photoinitiators being co-polymers of photoinitiator monomers and at least one further monomer, as well as photoinitiator monomers being intermediates in the preparation of such polymeric photoinitiators. Additionally, there is provided polyacrylate obtained by radical polymerization of at least one acrylate monomer (Ac) in the presence of such polymeric photoinitiators. In the photoinitiator monomers and polymeric photoinitiators, a photoinitiator moiety, a hydrolytic stable linker and two polymerisable functional groups are incorporated into the photoinitiator structure.
Synthesis and characterization of polymerizable one-component photoinitiator based on sesamol
Yang, Jinliang,Tang, Ruifen,Shi, Suqing,Nie, Jun
, p. 923 - 929 (2013/08/25)
Migration stability and biocompatibility are the crucial features for a photoinitiator or coinitiator used in UV curable formulations, especially when the cured product is in direct contact with food or human skin. To reduce the migration issues and increase the biocompatibility, a polymerizable one-component photoinitiator, 1-(1,3-benzodioxol-5-yloxy)-3-(4-benzoylphenoxy) propan-2-yl acrylate (BDOBPAc), based on sesamol and benzophenone has been synthesized. The photopolymerization induced by BDOBPAc was monitored by real-time infrared spectroscopy. The rate of decomposition and the migration stability of photoinitiators were studied by UV-Vis spectroscopy. The results showed that BDOBPAc is an effective free radical photoinitiator with good migration stability, which has great potential to be widely used in the food packing or biomedical fields.
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein
Jabeen, Ishrat,Pleban, Karin,Rinner, Uwe,Chiba, Peter,Ecker, Gerhard F.
experimental part, p. 3261 - 3273 (2012/06/01)
The drug efflux pump P-glycoprotein (P-gp) has been shown to promote multidrug resistance (MDR) in tumors as well as to influence ADME properties of drug candidates. Here we synthesized and tested a series of benzophenone derivatives structurally analogous to propafenone-type inhibitors of P-gp. Some of the compounds showed ligand efficiency and lipophilic efficiency (LipE) values in the range of compounds which entered clinical trials as MDR modulators. Interestingly, although lipophilicity plays a dominant role for P-gp inhibitors, all compounds investigated showed LipE values below the threshold for promising drug candidates. Docking studies of selected analogues into a homology model of P-glycoprotein suggest that benzophenones show an interaction pattern similar to that previously identified for propafenone-type inhibitors.
Photocrosslinked hydrogel blend surface coatings
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, (2008/06/13)
Hydrogel polymer blends including precursors and crosslinked forms of the compositions. The blends provide an improved approach to achieve high quality, uniform coatings with better commercial viability than other approaches including copolymerization. Applications include mass spectral analysis of biomolecular analytes such as proteins. Dextran and acrylamide systems are preferred. Benzophenone groups can be used as photocrosslinking groups. Photoinitiators are not needed. Functionalities which can selectively bind to biomolecular analytes are included.
Benzophenone derivative, ultraviolet absorbent and external preparation for skin
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, (2008/06/13)
Benzophenone derivatives expressed by the following general expression (1): wherein A in the above general expression (1) is a residual group obtained by removing one hydroxyl group from sugar or sugar alcohol, and B is a benzophenone group shown by the following general expression (2) STR1 wherein R1 through R10 each is expressed by hydrogen, hydroxyl group, an alkoxy group, or the aforesaid binder C, and at least one of them is the binder C. In the case of an alkoxy group, preferably the number of carbon atoms is 1 to 4. C is equivalent to --O--R-- (O is oxygen, R is a fatty chain, and the number of carbon atoms therein is preferably 1 to 4), or 1 mole of glycerin with one hydroxyl group therein bound to A and another hydroxyl group to B. The benzophenone derivatives according to the present invention have excellent capability to absorb ultraviolet rays as well as high compatibility with polar solvent. Also the external preparation for skin in which the benzophenone derivatives are mixed can be mixed in a polar base with wide availability for industrial purpose.
