134348-51-9Relevant academic research and scientific papers
Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1, adenosine receptor
Baraldi, Pier Giovanni,Romagnoli, Romeo,Pavani, Maria Giovanna,Del Carmen Nu?ez, Maria,Tabrizi, Mojgan Aghazadeh,Shryock, John C.,Leung, Edward,Moorman, Allan R.,Uluoglu, Canan,Iannotta, Valeria,Merighi, Stefania,Borea, Pier Andrea
, p. 794 - 809 (2003)
The current study describes the synthesis and biological evaluation of a novel series of 2-amino-3-naphthoylthiophenes, with variable modifications at the 4- and 5-position of the thiophene as well as the naphthoyl ring. Allosteric enhancer activity was m
Synthesis and Antimicrobial Evaluation of Novel Chiral 2-Amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridine Derivatives
Rossetti, Arianna,Bono, Nina,Candiani, Gabriele,Meneghetti, Fiorella,Roda, Gabriella,Sacchetti, Alessandro
, (2019)
New N-substituted-2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives were synthesized employing a convenient one-pot three-component method and their structures were characterized by 1H-NMR and single crystal X-ray diffraction analysis. All the synthesized compounds were in vitro screened for antimicrobial activity against Gram-positive (Sarcina lutea) and Gram-negative bacteria (Escherichia coli). In this work, we introduced a chiral residue on the tetrahydropyridine nitrogen, the hitherto the less investigated position on this pharmacophore in order to explore the effect. The antibacterial results showed that the synthesized compounds were active only against Gram-positive bacteria and the (R)-enantiomers displayed a greater antimicrobial potency than their (S)-counterparts. The structure–activity relationship here investigated may provide some interesting clues for future development of tetrahydrothienopyridine derivatives with higher antimicrobial activity.
Synthesis and Evaluation of Anti-inflammatory N-Substituted 3,5-Bis(2-(trifluoromethyl)benzylidene)piperidin-4-ones
Xie, Zixin,Zhang, Zaikui,Yu, Shufang,Cheng, Donghua,Zhang, Huan,Han, Chao,Lv, Handeng,Ye, Faqing
, p. 327 - 336 (2017/03/01)
A total of 24 N-substituted 3,5-bis(2-(trifluoromethyl)benzylidene)piperidin-4-one derivatives were synthesized via aldol condensation, and their anti-inflammatory activities were evaluated. These compounds were found to have no significant cytotoxicity a
Novel 2H-pyrazolo[4,3-c]hexahydropyridine derivatives: Synthesis, crystal structure, fluorescence properties and cytotoxicity evaluation against human breast cancer cells
Pang, Chuncheng,Sun, Chuanwen,Wang, Jing,Xiao, Di,Ding, Li,Bu, Hongfei
, p. 702 - 715 (2013/07/19)
A series of novel 2H-pyrazolo[4,3-c]hexahydropyridine derivatives (II) have been designed and synthesized. The target compounds have been identified by elemental analysis and spectral (1H NMR, IR, and MS) data and the absolute configuration of compound (II 1 ) was confirmed by single crystal X-ray diffraction. The cytotoxicity of the target compounds have been evaluated in vitro against two human breast cancer cell lines MCF-7 and MDA-MB-231 by MTT assay. Most compounds exhibited good inhibition, and compounds II 21 (IC50 = 4.7 μM for MCF-7 and IC50 = 9.3 μM for MDA-MB-231), II 33 (IC50 = 2.4 μM for MCF-7 and IC50 = 4.2 μM for MDA-MB-231) and II 40 (IC50 = 3.3 μM for MCF-7 and IC50 =8.6 μM for MDA-MB-231) displayed better inhibitory activity than 5-fluorouracil (IC 50 = 4.8 μM for MCF-7 and IC50 = 9.6 μM for MDA-MB-231, respectively). Flow cytometric analysis and DNA fragmentation suggest that II 33 is cytotoxic and able to induce the apoptosis of MCF-7 cells. The fluorescence properties of compounds II 1, II 6, II 11, II 16, II 23, II 28, and II 35 were also studied and compound II 28 afforded the highest photoluminescence quantum yield (38%).
1-[(4-HYDROXYPRIDIN-4-YL) METHYL]PYRIDINE-2(1H)-ONE DERIVATIVES, PREPARATION METHODS AND USES THEREOF
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Paragraph 0068, (2013/03/28)
Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof
1-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives, preparation methods and uses thereof
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Paragraph 0107, (2013/09/12)
Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. The above compounds have the dual activities of 5-hydroxytryptamine 1A receptor ligand and selective serotonin reuptake inhibitor. The preparation methods of the above compounds, the uses of these compounds for the prevention or treatment of nervous system diseases related to 5-hydroxytryptamine system dysfunction and the pharmaceutical compositions containing these compounds are also provided.
Synthesis, crystal structure and anticancer activities of tetrahydropyrido[4,3-d]dihydropyrimidine-2-thiones
Ding, Li,Xue, Sijia,Li, Jing,Xiao, Di,Wang, Jing,Hao, Zhibing,Pang, Chuncheng
, p. 2509 - 2516 (2013/01/15)
A new series of tetrahydropyrido[4,3-d]dihydropyrimidine-2-thiones (3a-3x) were designed and synthesized. Their structures were confirmed by1H NMR, IR, MS and elemental analysis, and the conformation of compound 3j was confirmed by X-ray diffraction. Preliminary bioassays indicated that most of the target compounds presented good antiproliferative activities against leukemic K562 cells, ovarian cancer HO-8910 cells and liver cancer SMMC-7721 cells in vitro. Among them the compounds 3i and 3m afford the best activity, the IC 50 of them were 3.22 and 3.65 iμg/mL against leukemic K562 cells, respectively, which were lower than the anticancer drug of clinical practice 5-FU (IC50=8.56 iμg/mL). Preliminary mechanism of action studies revealed that compound 3i caused DNA fragmentation and activated caspase-3/7 in leukemic K562 cells. A new series of tetrahydropyrido[4,3-d] dihydropyrimidine-2-thiones (3a-3x) were synthesized and the conformation of compound 3j was confirmed by X-ray diffraction. Preliminary bioassays indicated that most of the target compounds presented good antiproliferative activities against leukemic K562 cells, ovarian cancer HO-8910 cells and liver cancer SMMC-7721 cells in vitro. Preliminary mechanism of action studies revealed that compound 3i caused DNA fragmentation and activated caspase-3/7 in leukemic K562 cells. Copyright
N-(substituted benzyl)-3,5-bis(benzylidene)-4-piperidones: Synthesis and preliminary anti-leukemia activity (I)
Wang, Jing,Meng, Wen,Ni, Zhenjie,Xue, Sijia
, p. 2109 - 2113 (2012/03/11)
A series of novel N-(substituted benzyl)-3,5-bis(benzylidene)-4-piperidones 5a-5o were synthesized with substituted benzylamines as raw materials via a series of Michael addition, Dieckmann condensation, hydrolysis decarboxylation and aldol condensation.
NOVEL COMPOUNDS USEFUL AS CC CHEMOKINE RECEPTOR LIGANDS
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Page/Page column 82, (2010/07/08)
The present invention relates to novel morpholine, oxazapane and piperidine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
NOVEL BENZODIOXANE AND BENZOXAZINE DERIVATIVES USEFUL AS CC CHEMOKINE RECEPTOR LIGANDS
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Page/Page column 86, (2010/06/22)
The present invention relates to benzodioxane and benzoxazine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
