20248-73-1Relevant academic research and scientific papers
Hyperbranched poly(ether amine) (hPEA) as novel backbone for amphiphilic one-component type-II polymeric photoinitiators
Li, Tiantian,Su, Zhilong,Xu, Hongjie,Jiang, Xuesong,Ma, Xiaodong,Yin, Jie
, p. 451 - 455 (2018)
To make photoinitiators (PI) to be polymeric and water-soluble is an effective approach to develop the high efficient photoinitiator systems with low-migration, low-toxic and environment-friend. We developed a series of novel amphiphilic hyperbranched pol
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 (2015/11/09)
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.
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.
