143773-71-1Relevant articles and documents
Graphene Oxide Promotes Site-Selective Allylic Alkylation of Thiophenes with Alcohols
Favaretto, Laura,An, Juzeng,Sambo, Marco,De Nisi, Assunta,Bettini, Cristian,Melucci, Manuela,Kovtun, Alessandro,Liscio, Andrea,Palermo, Vincenzo,Bottoni, Andrea,Zerbetto, Francesco,Calvaresi, Matteo,Bandini, Marco
, p. 3705 - 3709 (2018)
The graphene oxide (GO) assisted allylic alkylation of thiophenes with alcohols is presented. Mild reaction conditions and a low GO loading enabled the isolation of a range of densely functionalized thienyl and bithienyl compounds in moderate to high yields (up to 90%). The cooperative action of the Br?nsted acidity, epoxide moieties, and π-surface of the 2D-promoter is highlighted as crucial in the reaction course of the present Friedel-Crafts-type protocol.
Synthesis of α-aminonitriles with benzimidazolic and theophyllinic backbones using the strecker reaction
Khalafi-Nezhad, Ali,Divar, Masoumeh,Panahi, Farhad
, p. 10902 - 10908 (2013)
An example of the application of the Strecker reaction in the synthesis of a new class of α-aminonitriles with benzimidazole and theophylline backbones has been developed. For the synthesis of these compounds, first 4-hydroxybenzaldehyde was reacted with
Synthesis of Imidazole and Theophylline Derivatives Incorporating Pyrimidine-Fused Heterocycles Using Magnetic Nanoparticles-Supported Tungstic Acid (MNP-TA) Catalyst
Divar, Masoumeh,Panahi, Farhad,Shariatipour, Sayedeh Rojin,Khalafi-Nezhad, Ali
, p. 660 - 669 (2017)
In the current study, divers pyrimidine-fused heterocycles containing an imidazole, benzimidazole, or theophylline moieties were synthesized. For the synthesis of this category of compounds, first, some new bromo-substituted aldehydes (BSAs) were synthesi
Synthesis of hantzsch adducts as cholinesterases and calcium flux inhibitors, antioxidants and neuroprotectives
Angona, Irene Pachón,Martin, Helene,Daniel, Solene,Moraleda, Ignacio,Bonet, Alexandre,Wnorowski, Artur,Maj, Maciej,Jozwiak, Krzysztof,Iriepa, Isabel,Refouvelet, Bernard,Marco-Contelles, José,Ismaili, Lhassane
, p. 1 - 19 (2020/10/29)
We report herein the design, synthesis, biological evaluation, and molecular modelling of new inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), able to block Ca+2 channels also showing antioxidant and neuroprotective activities. The new MTDL, dialkyl 2,6-dimethyl-4-(4-((5-aminoalkyl)oxy)phenyl)-1,4-dihydropyridine-3,5-dicarboxylate 3a-p, have been obtained via Hantzsch reaction from appropriate and commercially available precursors. Pertinent biological analysis has prompted us to identify MTDL 3h [dimethyl-4-(4-((5-(4-benzylpiperidin-1-yl)pentyl)oxy)phenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate] as an attractive inhibitor of AChE (1.8 μM) and BuChE (2 μM), Ca+2 channel antagonist (47.72% at 10 μM), and antioxidant (2.54 TE) agent, showing significant neuroprotection 28.68% and 38.29% against H2 O2, and O/R, respectively, at 0.3 μM, thus being considered a hit-compound for further investigation in our search for anti-Alzheimer’s disease agents.
A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties
Canale, Vittorio,Grychowska, Katarzyna,Kurczab, Rafa?,Ryng, Mateusz,Keeri, Abdul Raheem,Sata?a, Grzegorz,Olejarz-Maciej, Agnieszka,Koczurkiewicz, Paulina,Drop, Marcin,Blicharz, Klaudia,Piska, Kamil,P?kala, El?bieta,Janiszewska, Paulina,Krawczyk, Martyna,Walczak, Maria,Chaumont-Dubel, Severine,Bojarski, Andrzej J.,Marin, Philippe,Popik, Piotr,Zajdel, Pawe?
supporting information, (2020/09/21)
The complex etiology of Alzheimer's disease has initiated a quest for multi-target ligands to address the multifactorial causes of this neurodegenerative disorder. In this context, we designed dual-acting 5-HT6 receptor (5-HT6R) anta
Allylic and Allenylic Dearomatization of Indoles Promoted by Graphene Oxide by Covalent Grafting Activation Mode
Lombardi, Lorenzo,Bellini, Daniele,Bottoni, Andrea,Calvaresi, Matteo,Monari, Magda,Kovtun, Alessandro,Palermo, Vincenzo,Melucci, Manuela,Bandini, Marco
supporting information, p. 10427 - 10432 (2020/07/24)
The site-selective allylative and allenylative dearomatization of indoles with alcohols was performed under carbocatalytic regime in the presence of graphene oxide (GO, 10 wt percent loading) as the promoter. Metal-free conditions, absence of stoichiometric additive, environmentally friendly conditions (H2O/CH3CN, 55 °C, 6 h), broad substrate scope (33 examples, yield up to 92 percent) and excellent site- and stereoselectivity characterize the present methodology. Moreover, a covalent activation model exerted by GO functionalities was corroborated by spectroscopic, experimental and computational evidences. Recovering and regeneration of the GO catalyst through simple acidic treatment was also documented.
ANTI-ENTEROVIRUS 71 THIADIAZOLIDINE DERIVATIVE
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Paragraph 0106-0107; 0374-0375, (2017/03/28)
Disclosed is a novel anti-enterovirus 71 (EV71) 1,2,5-thiadiazolidine-1,1-dioxide derivative or a pharmaceutically acceptable salt thereof; and specifically, a compound represented by formula (II) or a pharmaceutically acceptable salt thereof.
Synthesis of new α-aminophosphonate derivatives incorporating benzimidazole, theophylline and adenine nucleobases using l-cysteine functionalized magnetic nanoparticles (LCMNP) as magnetic reusable catalyst: Evaluation of their anticancer properties
Bahrami, Foroogh,Panahi, Farhad,Daneshgar, Fatemeh,Yousefi, Reza,Shahsavani, Mohammad Bagher,Khalafi-Nezhad, Ali
, p. 5915 - 5924 (2016/02/05)
A new class of structurally diverse α-aminophosphonate derivatives containing benzimidazole, theophylline and adenine heterocycles were synthesized using a simple and efficient strategy. This class of α-aminophosphonates was synthesized using the reaction
Hybrid pharmacophore design and synthesis of naphthalimide-benzimidazole conjugates as potential anticancer agents
Kamal, Ahmed,Kumar, Pogula Praveen,Khan, Mohammed Naseer Ahmed,Sheshadri, Bobburi Naga,Srinivas, Olepu
, p. 374 - 384 (2015/06/22)
Naphthalimide-benzimidazole conjugates were prepared using two different types of spacer units; either a simple alkane chain or a substituted piperazine moiety with variable alkyl side chains. Each set of conjugates was evaluated for their in vitro antica
Multitarget-directed resveratrol derivatives: Anti-cholinesterases, anti-β-amyloid aggregation and monoamine oxidase inhibition properties against Alzheimer's disease
Pan, Long-Fei,Wang, Xiao-Bing,Xie, Sai-Sai,Li, Su-Yi,Kong, Ling-Yi
supporting information, p. 609 - 616 (2014/05/06)
Considering the complex pathogenesis factors of Alzheimer's disease (AD), the multitarget-directed ligand strategy is expected to provide superior effects to fight AD, instead of the classic one-drug-one-target strategy. Resveratrol, exhibiting important properties against AD, was suggested to be used as a starting compound for the treatment of AD. Based on these reasons, a series of resveratrol derivatives were designed, synthesized and biologically evaluated. Among them, compound 6r, exhibiting moderate cholinesterase inhibition activity (AChE, IC50 = 6.55 μM; BuChE, IC50 = 8.04 μM; SI = 1.23), significant inhibition of Aβ42 aggregation (57.78%, at 20 μM) and acceptable inhibitory activity against monoamine oxidases (MAO-A, IC50 = 17.58 μM; MAO-B, IC50 = 12.19 μM), was a potential anti-Alzheimer agent with balanced activities. Consequently, this study provided useful information for further development of resveratrol derivatives as multitarget-directed agents for AD therapy. This journal is the Partner Organisations 2014.