2138-33-2Relevant academic research and scientific papers
Metal-free synthesis of β-aminoketones by the reductive hydroamination of ynones
Fu, Rui,Liu, Yu,Wu, Tao,Zhang, Xinyu,Zhu, Yang,Luo, Jiangbin,Zhang, Zhengyu,Jiang, Yaojia
, p. 3525 - 3528 (2022/03/31)
This study describes a cascade method for the synthesis of β-aminoketones through the reductive hydroamination of alkynes under very mild metal-free conditions. It allows for the rapid conversion of ynones and amines into corresponding β-aminoketones with a broad substrate scope and diverse functionalities. This straightforward and easy-to-handle reaction process can be successfully applied for the synthesis of Proroxan and Propipocaine, offering a potential option for the synthesis of drug molecules with the β-aminoketone skeleton.
SMALL MOLECULE CMKLR1 ANTAGONISTS IN INFLAMMATORY DISEASE
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Paragraph 0199; 0230; 0232; 0246, (2020/12/01)
α-NETA analogs are provided for the treatment of inflammatory disease.
Synthesis and pharmacological investigation of aralkyl diamine derivatives as potential triple reuptake inhibitors
Zheng, Yong-Yong,Weng, Zhi-Jie,Xie, Peng,Zhu, Mei-Yu,Xing, Long-Xuan,Li, Jian-Qi
, p. 219 - 234 (2014/09/17)
A series of aralkyl diamine derivatives were designed, synthesized, and evaluated for their triple reuptake inhibitory abilities. Compounds 18c (5-HT, NE, DA, IC50 = 389, 69, 238 nM), 36a (5-HT, NE, DA, IC50 = 378, 477, 247 nM), and
GAMMA-DIKETONES AS WNT/BETA -CATENIN SIGNALING PATHWAY ACTIVATORS
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Paragraph 1714; 1715; 1716; 1729, (2014/09/03)
The present disclosure provides γ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANT
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Paragraph 0030; 0106, (2013/03/28)
Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
Design of tRNALys3 Ligands: Fragment evolution and linker selection guided by NMR spectroscopy
Chung, Florence,Tisne, Carine,Lecourt, Thomas,Seijo, Bili,Dardel, Frederic,Micouin, Laurent
scheme or table, p. 7108 - 7116 (2010/04/05)
A fragment-based approach for the synthesis of ligands of tRNA Lys3, the HIV reverse-transcription primer, is described. The use of NMR spectroscopy has proved to be very useful in this approach, not only to detect lowaffinity complexes between small compounds and RNA, but also to provide information on their binding mode and on the way they can be connected. This NMR-spectroscopy-guided analysis enabled us to design micromolar ligands after the optimisation and connection of millimolar fragments with an appropriate linker. The influence of the linker region on the binding affinity and selectivity outlines the importance of having a flexible assemblage strategy with a variety of linkers in such an approach. 2009 Wiley-VCH Verlag GmbH & Co. KGaA.
NMR-guided fragment-based approach for the design of tRNALys3 ligands
Chung, Florence,Tisne, Carine,Lecourt, Thomas,Dardel, Frederic,Micouin, Laurent
, p. 4489 - 4491 (2008/03/27)
Two in one: Two ligands for tRNALys3 that were identified from a compound library by flow-injection NMR spectroscopic screening and found to have millimolar dissociation constants (on the left in the picture) inspired the fragment-based synthesis of a new family of ligands with the general structural features of both initial compounds. Ligand 1 of this family is a selective D-stem binder of tRNALys3 with a micromolar Kd value.
A convenient alternative route to β-aminoketones
San Martin,De Marigorta,Dominguez
, p. 2255 - 2264 (2007/10/02)
Enaminones has been prepared and submitted to conjugate reduction with LAH and the system Al2O3/R2NH to give β-aminoketones. The latter tandem amination system has also been applied in the Mannich reaction, improving the synthesis of several new diaryl β-aminoketones. Besides, the sequential use of DMFDMA and LAH-CuI on deoxybenzoins furnishes a new route for the synthesis of enones.
Evaluation of some Mannich bases derived from substituted acetophenones against P-388 lymphocytic leukemia and on respiration in isolated rat liver mitochondria
Dimmock,Shyam,Hamon,Logan,Raghavan,Harwood,Smith
, p. 887 - 894 (2007/10/02)
Series of 3-dimethylamino-1-aryl-1-propanone hydrobromides (IV) and 3-dimethylamino-2-dimethylaminomethyl-1-aryl-1-propanone dihydrobromides (V) were synthesized. Evaluation of these derivatives against P-388 lymphocytic leukemia growth revealed that two compounds show promise as antineoplastic agents. Compounds of the V series were unstable in phosphate buffer (in contrast to series IV), and when the same nuclear substituent was present in both series of compounds, V was ~ 100 times more active than IV in both the stimulation and inhibition of respiration of mitochondria isolated from rat liver cells. Representatives from both series showed that respiration in mitochondria was affected by changing the pH of the aqueous buffer from 7.4 to 6.9 or 6.4 and by reducing the temperature from 37° to 20°. The compounds showed reactivity toward a biomimetic thiol.
