404-95-5Relevant academic research and scientific papers
β-Amino alcohols from anilines and ethylene glycol through heterogeneous Borrowing Hydrogen reaction
Llabres-Campaner, Pedro J.,Ballesteros-Garrido, Rafael,Ballesteros, Rafael,Abarca, Belén
supporting information, p. 5552 - 5561 (2017/08/22)
Borrowing Hydrogen (BH), also called Hydrogen Autotransfer (HA), reaction with neat ethylene glycol represents a key step in the preparation of β-amino alcohols. However, due to the stability of ethylene glycol, mono-activation has rarely been achieved. Herein, a combination of Pd/C and ZnO is reported as heterogeneous catalyst for this BH/HA reaction. This system results in an extremely air and moisture stable, and economic catalyst able to mono-functionalize ethylene glycol in water, without further activation of the diol. In this work, different diols and aromatic amines have been explored affording a new approach towards amino alcohols. This study reveals how the combination of two solid species can afford interesting catalytic properties in heterogeneous phase. ZnO activates ethylene glycol while Pd/C is the responsible of the BH/HA cycle. This catalytic system has also been found useful to dehydrogenate indoles affording indolines that undergo in situ BH/HA cycle prior to re-aromatization, representing a tandem heterogeneous process.
Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors
Yin, Yan,Zheng, Ke,Eid, Nibal,Howard, Shannon,Jeong, Ji-Hak,Yi, Fei,Guo, Jia,Park, Chul Min,Bibian, Mathieu,Wu, Weilin,Hernandez, Pamela,Park, Hajeung,Wu, Yuntao,Luo, Jun-Li,Lograsso, Philip V.,Feng, Yangbo
, p. 1846 - 1861 (2015/04/21)
The discovery/optimization of bis-aryl ureas as Limk inhibitors to obtain high potency and selectivity and appropriate pharmacokinetic properties through systematic SAR studies is reported. Docking studies supported the observed SAR. Optimized Limk inhibitors had high biochemical potency (IC50 400-fold), potent inhibition of cofilin phosphorylation in A7r5, PC-3, and CEM-SS T cells (IC50 1 μM), and good in vitro and in vivo pharmacokinetic properties. In the profiling against a panel of 61 kinases, compound 18b at 1 μM inhibited only Limk1 and STK16 with ≥80% inhibition. Compounds 18b and 18f were highly efficient in inhibiting cell-invasion/migration in PC-3 cells. In addition, compound 18w was demonstrated to be effective on reducing intraocular pressure (IOP) on rat eyes. Taken together, these data demonstrated that we had developed a novel class of bis-aryl urea derived potent and selective Limk inhibitors.
TRICYCLIC NITROGEN CONTAINING COMPOUNDS AND THEIR USE AS ANTIBACTERIALS
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, (2009/12/27)
Compounds of Formula (I) or a pharmaceutically acceptable salt or N-oxide thereof; Formula (I) (relative stereochemistry shown) wherein: Z1, Z2 , L are as defined, U represents a cyclic group selected from: phenyl, pyridyl, pyridazin
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists
Goodacre, Caroline J.,Bromidge, Steven M.,Clapham, David,King, Frank D.,Lovell, Peter J.,Allen, Mike,Campbell, Lorraine P.,Holland, Vicky,Riley, Graham J.,Starr, Kathryn R.,Trail, Brenda K.,Wood, Martyn D.
, p. 4989 - 4993 (2007/10/03)
Bisaryl cyclic ureas have been identified as high affinity 5-HT 2C receptor antagonists with selectivity over 5-HT2A and 5-HT2B. Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function in rodents.
4-(Quinolin-2-yl-methoxy)-phenyl-acetic acid derivatives
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, (2008/06/13)
4-(Quinolin-2-yl-methoxy)-phenyl-acetic acid derivatives are prepared by reacting quinoline-methoxy-phenyl-acetic acids with the corresponding glycinol derivatives, if appropriate with activation of the carboxylic acid function. The new compounds are suit
