5710-32-7Relevant academic research and scientific papers
Synthesis and Mesomorphic Properties of Novel Bent-shaped Naphthyl Diketones
Buljan, An?ela,Kne?evi?, Anamarija,Dokli, Irena,Lesac, Andreja
, p. 173 - 179 (2019/12/12)
The synthesis and liquid-crystalline properties are reported for novel naphthyl-based diketones incorporating variant terminal chains and lateral fluoro- substitution. Newly prepared materials exhibit a broad temperature range of the nematic phase. The study demonstrates how subtle structural modifications can be exploited to alter the efficiency of molecular packing and consequently the thermal behaviour.
N -pyridyl and pyrimidine benzamides as KCNQ2/Q3 potassium channel openers for the treatment of epilepsy
Amato, George,Roeloffs, Rosemarie,Rigdon, Greg C.,Antonio, Brett,Mersch, Theresa,McNaughton-Smith, Grant,Wickenden, Alan D.,Fritch, Paul,Suto, Mark J.
supporting information; experimental part, p. 481 - 484 (2011/08/22)
A series of N-pyridyl benzamide KCNQ2/Q3 potassium channel openers were identified and found to be active in animal models of epilepsy and pain. The best compound 12 [ICA-027243, N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide] has an EC50 of 0.38 μM and is selective for KCNQ2/Q3 channels. This compound was active in several rodent models of epilepsy and pain but upon repeated dosing had a number of unacceptable toxicities that prevented further development. On the basis of the structure-activity relationships developed around 12, a second compound, 51, [N-(2-chloro-pyrimidin-5-yl)-3,4-difluoro- benzamide, ICA-069673], was prepared and advanced into a phase 1 clinical study. Herein, we describe the structure-activity relationships that led to the identification of compound 12 and to the corresponding pyrimidine 51.
Small-Molecule Choline Kinase Inhibitors as Anti-Cancer Therapeutics
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Page/Page column 23; 27-28, (2011/10/31)
Small molecule choline kinase inhibitors having the following formula: are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting choline kinase enzymatic activity, and methods of treating tumors by administering an effective amount of a Formula I compound.
