5554-64-3Relevant 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.
Fluoxetine scaffold to design tandem molecular antioxidants and green catalysts
Bortoli, Marco,Gianoncelli, Alessandra,Ongaro, Alberto,Orian, Laura,Oselladore, Erika,Ribaudo, Giovanni,Zagotto, Giuseppe
, p. 18583 - 18593 (2020/06/08)
Fluoxetine finds application in the treatment of depression and mood disorders. This selective serotonin-reuptake inhibitor (SSRI) also contrasts oxidative stress by direct ROS scavenging, modulation of the endogenous antioxidant defense system, and/or enhancement of the serotonin antioxidant capacity. We synthesised some fluoxetine analogues incorporating a selenium nucleus, thus expanding its antioxidant potential by enabling a hydroperoxides-inactivating, glutathione peroxidase (GPx)-like activity. Radical scavenging and peroxidatic activity were combined in a water-soluble, drug-like, tandem antioxidant molecule. Selenofluoxetine derivatives were reacted with H2O2in water, and the mechanistic details of the reaction were unravelled combining nuclear magnetic resonance (NMR), electrospray ionisation-mass spectrometry (ESI-MS) and quantum chemistry calculations. The observed oxidation-elimination process led to the formation of seleninic acid and cinnamylamine in atrans-selective manner. This mechanism is likely to be extended to other substrates for the preparation of unsaturated cinnamylamines.
SMALL MOLECULE CMKLR1 ANTAGONISTS IN INFLAMMATORY DISEASE
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Paragraph 0201; 0264-0265; 0267, (2020/12/01)
α-NETA analogs are provided for the treatment of inflammatory disease.
3-[(BENZO[D][1,3]DIOXOLAN-4-YL)-OXY]-3-ARYLPROPYLAMINE TYPE COMPOUNDS AND APPLICATIONS THEREOF
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Paragraph 0066, (2018/02/02)
The present invention relates to 3-[(benzo[d][1,3]dioxolan-4-yl)-oxy]-3-arylpropylamine compounds of formula I or pharmaceutically acceptable salts thereof and use thereof. The compound may be used to prepare an antidepressant agent.
Probing the effect of heterocycle-bonding in PNX-type ruthenium pre-catalysts for reactions involving H2
Xu,Langer
supporting information, p. 16785 - 16790 (2015/10/05)
A series of ruthenium(ii) complexes with three novel PNX-type pincer ligands is reported, in which X denotes a heterocyclic donor group (PNX = Ph2PCH2CH2N(H)CH2-X, X = 2-pyridyl, 2-furanyl, 2-thiophenyl or 2-pyrrolyl). The reaction of [(Ph3P)3RuCl2] with one equivalent of ligand leads to the trans-dichloro complexes [(PNX)RuCl2(PPh3)] (1-4) for all ligands, whereas the complexation of [(Ph3P)3Ru(H)(Cl)(CO)] results in different types of complexes. The variation of the heterocyclic donor group is in line with different binding properties and a labilization of this group. Investigations on the catalytic activity of different types of ruthenium(ii) complexes in hydrogenation and dehydrogenation reactions reveal that more labile bound heterocycle donors result in a decrease of catalytic productivity and activity.
Design of novel multiple-acting ligands towards SERT and 5-HT2C receptors
éliás, Olivér,ágai-Csongor, éva,Domány, Gy?rgy,Keseru, Gy?rgy Miklós,Gere, Anikó,Kiss, Béla,Hellinger, éva,Vastag, Mónika,Gyertyán, István
, p. 2118 - 2122 (2014/05/06)
This Letter describes our attempts to elaborate dually acting compounds possessing serotonin re-uptake transporter inhibitor and serotonin 5-HT 2C receptor antagonist properties. A novel series of 1,3-diphenylureas and N-phenylbenzamides have thus been prepared and evaluated. Based on its in vitro and in vivo activities, as well as pharmacokinetic profile, compound 16a was identified as a lead compound. The synthesis and structure-activity relationship of this series of compounds is presented herein.
Acid-catalyzed ether rearrangement: Total synthesis of isomimosifoliol and (±)-dihydromimosifoliol
Arava, Veera Reddy,Malreddy, Sashibhushan,Thummala, Sreenivasulu Reddy
, p. 3545 - 3552,8 (2020/08/31)
An acid-catalyzed rearrangement of benzyl phenyl ethers to diphenylmethane derivatives, followed by salt formation and Hofmann elimination, is a simple method for the syntheses of isomimosifoliol and dihydromimosifoliol.
Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and mannich bases: Interaction with DNA
Tóth, Katalin,Wenzel, Nicole I.,Chavain, Natascha,Wang, Yulin,Friebolin, Wolfgang,Maes, Louis,Pradines, Bruno,Lanzer, Michael,Yardley, Vanessa,Brun, Reto,Herold-Mende, Christel,Biot, Christophe,Davioud-Charvet, Elisabeth
scheme or table, p. 3214 - 3226 (2010/10/19)
The synthesis and biological evaluation of new organic and organometallic dual drugs designed as potential antimalarial agents are reported. A series of 4-aminoquinoline-based Mannich bases with variations in the aliphatic amino side chain were prepared via a three-steps synthesis. These compounds were also tested against chloroquine-susceptible and chloroquine-resistant strains of Plasmodium falciparum and assayed for their ability to inhibit the formation of β-hematin in vitro using a colorimetric β-hematin inhibition assay. Several compounds showed a marked antimalarial activity, with IC50 and IC90 values in the low nM range but also a high cytotoxicity against mammalian cells, in particular a highly drug-resistant glioblastoma cell line. The newly designed compounds revealed high DNA binding properties, especially for the GC-rich domains. Altogether, these dual drugs seem to be more appropriate to be developed as antiproliferative agents against mammalian cancer cells than Plasmodium parasites.
AN IMPROVED PROCESS FOR SYNTHESIZING HIGHLY PURE ATOMOXETINE
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Page/Page column 11, (2009/12/27)
The present invention relates to a process for the preparation of highly pure atomoxetine of formula (I) and pharmaceutically acceptable salts thereof Formula (I) The present invention also aims at novel processes for the preparation and purification of intermediates involved in the process of the present invention.
INHIBITORS OF AKT ACTIVITY
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, (2008/06/13)
Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
