290365-83-2Relevant academic research and scientific papers
Synthesis and biological assessment of 4,1-benzothiazepines with neuroprotective activity on the Ca2+ overload for the treatment of neurodegenerative diseases and stroke
Arribas, Raquel L.,Braun-Cornejo, María,De Los Ríos, Cristóbal,Estrada-Valencia, Martín,Moreno-Castro, Manuel,Pérez-Marín, Raquel,Rubio-Alarcón, Marcos,Viejo, Lucía
supporting information, (2021/08/09)
In excitable cells, mitochondria play a key role in the regulation of the cytosolic Ca2+ levels. A dysregulation of the mitochondrial Ca2+ buffering machinery derives in serious pathologies, where neurodegenerative diseases highlight. Since the mitochondrial Na+/Ca2+ exchanger (NCLX) is the principal efflux pathway of Ca2+ to the cytosol, drugs capable of blocking NCLX have been proposed to act as neuroprotectants in neuronal damage scenarios exacerbated by Ca2+ overload. In our search of optimized NCLX blockers with augmented drug-likeness, we herein describe the synthesis and pharmacological characterization of new benzothiazepines analogues to the first-in-class NCLX blocker CGP37157 and its further derivative ITH12575, synthesized by our research group. As a result, we found two new compounds with an increased neuroprotective activity, neuronal Ca2+ regulatory activity and improved drug-likeness and pharmacokinetic properties, such as clog p or brain permeability, measured by PAMPA experiments.
Rapid construction of an effective antifouling layer on a Au surface via electrodeposition
Li, Bor-Ran,Shen, Mo-Yuan,Yu, Hsiao-Hua,Li, Yaw-Kuen
supporting information, p. 6793 - 6796 (2014/06/23)
A new approach to immobilize zwitterionic molecules rapidly and highly efficiently on a gold surface applies aniline-based electrodeposition. The zwitterion-functionalized antifouling surface enables a decrease of the adsorption of non-specific proteins by 95% from fetal bovine serum (FBS, 10%). This journal is the Partner Organisations 2014.
Phosphoramidate tantalum complexes for room-temperature C-H functionalization: Hydroaminoalkylation catalysis
Garcia, Pierre,Lau, Ying Yin,Perry, Mitchell R.,Schafer, Laurel L.
supporting information, p. 9144 - 9148 (2013/09/12)
A cooled reaction: Phosphoramidate-ClTaMe3 complexes promote the first example of room-temperature hydroaminoalkylation catalysis. This reaction can be realized under solvent-free conditions and with challenging substrates such as styrenes and dialkyl amines. When using a vinylsilane substrate, for the first time the linear regioisomer is obtained preferentially using a Group5 metal. TBS=tert-butyldimethylsilyl, TMS=trimethylsilyl. Copyright
Palladium-catalyzed amidation of aryl halides using 2-dialkylphosphino- 2′-alkoxyl-1,1′-binaphthyl as ligands
Ma, Fangfang,Xie, Xiaomin,Zhang, Lei,Peng, Zhiyong,Ding, Lina,Fu, Lei,Zhang, Zhaoguo
experimental part, p. 5279 - 5285 (2012/08/07)
Palladium-catalyzed intermolecular C-N bond-forming reactions between aryl halides and amides are described using 2-dialkylphosphino-2′-alkoxyl-1, 1′-binaphthyl, which is both bulky and electron-rich, as the ligand. A variety of amides, including aliphatic and aromatic primary amides, lactams, and carbamates, were viable substrates for the amidation, which exhibited good functional group compatibility. By tuning the substituents at the 2,2′-position of 1,1′-binaphthyl of the ligand, the palladium-catalyzed amidation of bulky aryl halides was realized and this coupling reaction was used to synthesize 2-amino-2′-methoxy-1,1′- binaphthyl in high yield.
Guanidine and 2-aminoimidazoline aromatic derivatives as α2-adrenoceptor ligands: Searching for structure-activity relationships
Rodriguez, Fernando,Rozas, Isabel,Ortega, Jorge E.,Erdozain, Amaia M.,Meana, J. Javier,Callado, Luis F.
supporting information; experimental part, p. 601 - 609 (2009/11/30)
In this paper, we report the synthesis of three new 2-aminoimidazoline (compounds 4b, 5b, and 6b) and three new guanidine derivatives (compounds 7b, 8b, and 9b) as potential α2-adrenoceptor antagonists for the treatment of depression. Their pha
Room-temperature Pd-catalyzed amidation of aryl bromides using tert-butyl carbamate
Bhagwanth, Swapna,Waterson, Alex G.,Adjabeng, George M.,Hornberger, Keith R.
supporting information; experimental part, p. 4634 - 4637 (2009/09/08)
(Chemical Equation Presented) The scope of Pd-catalyzed synthesis of N-Boc-protected anilines from aryl bromides and commercially available tertbutyl carbamate is described. For the first time, this process can be conducted at room temperature (17-22°C) u
