- Synthesis and characterization of poly(3-thiophene acetic acid)/Fe 3O4 nanocomposite
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Poly(3-thiophene acetic acid)/Fe3O4 nanocomposite is synthesized by the precipitation of Fe3O4 in the presence of poly(3-thiophene acetic acid) (P3TAA). Structural, surface, morphological, thermal properties and conductivity characterization/evaluation of the nanocomposite were performed by XRD, FT-IR, TEM, TGA, and conductivity measurements, respectively. The capping of P3TAA around Fe3O 4 nanoparticles was confirmed by FT-IR spectroscopy, the interaction being via bridging oxygens of the carboxylate and the nanoparticle surface through bidentate binding. The crystallite and particle size were obtained as 9 ± 2 nm and 11 ± 1 nm from XRD line profile fitting and TEM image analysis, respectively, which reveal nearly single crystalline nature of Fe 3O4 nanoparticles. Magnetization measurements reveal that P3TAA coated magnetite particles do not saturate at higher fields. There is no coercivity and remanence revealing superparamagnetic character. Magnetic particle size calculated from the theoretical fitting as 9.1 nm which coincides the values determined from TEM micrographs and XRD line profile fitting. The comparison to the TEM particle size reveals slightly modified magnetically dead nanoparticle surface.
- Aydin,Durmus,Kavas,Esat,S?zeri,Baykal,Yilmaz,Toprak
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- Synthesis of functionalized thiophenes for the preparation of conducting polymer films with complexing properties
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Four series of novel substituted thiophenes (Schiff bases, esters, amides, and amino acids) have been synthesized and tested for their ability to form conducting polymer films via cyclic voltammetry in order to obtain electrochemical sensors for metal cations. The influence of the nature and size of the substituents on the electropolymerizability of the monomers has been studied. Copyright Taylor & Francis Group, LLC.
- Brembilla,Collard,Henry,Jadamiec,Lapkowski,Matlengiewicz,Rodehueser
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- Preparation and electrochemical performance of TEMPO-modified polyterthiophene electrode obtained by electropolymerization
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A novel monomer of terthiophene with a side chain TEMPO, 4-(2,5-di(thiophen-2-yl)thiophen-3-yl)acetyl-oxy-2,2,6,6-tetramethylpiperidin-1-yloxy (TT-TEMPO) was successfully synthesized. Its corresponding polymer PTT-TEMPO was prepared via electrochemical polymerization on Pt electrode in boron trifluoride diethyl etherate solution. PTT-TEMPO film showed a uniform network structure. Compared with bare Pt electrode, PTT-TEMPO electrode exhibited high electrocatalytic performance for oxidation of benzyl alcohol in the presence of 2,6-lutidine under similar conditions. Benzyl alcohol was selectively oxidized to benzaldehyde based on in situ FTIR analysis.
- Niu, Pengfei,Cai, Yanchao,Guo, Ming,Shen, Zhenlu,Li, Meichao
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- syn-Selective Michael Reaction of α-Branched Aryl Acetaldehydes with Nitroolefins Promoted by Squaric Amino Acid Derived Bifunctional Br?nsted Bases
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Here we describe a direct access to 2,2,3-trisubstituted syn γ-nitroaldehydes by addition of α-branched aryl acetaldehydes to nitroolefins promoted by a cinchona based squaric acid-derived amino acid peptide. Different α-methyl arylacetaldehydes react with β-aromatic and β-alkyl nitroolefins to afford the Michael adducts in high enantioselectivity and syn-selectivity. NMR experiments and DFT calculations predict the reaction to occur through the intermediacy of E-enolate. The interaction between the substrates and the catalyst follows Pápai's model, wherein an intramolecular H-bond interaction in the catalyst between the NH group of one of the tert-leucines and the squaramide oxygen seems to be key for discrimination of the corresponding reaction transition states.
- Campano, Teresa E.,García-Urricelqui, Ane,Mielgo, Antonia,Palomo, Claudio,de Cózar, Abel
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supporting information
p. 3604 - 3612
(2021/07/26)
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- Green Esterification of Carboxylic Acids Promoted by tert-Butyl Nitrite
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In this work, the green esterification of carboxylic acids promoted by tert-butyl nitrite has been well developed. This transformation is compatible with a broad range of substrates and exhibits excellent functional group tolerance. Various drugs and substituted amino acids are applicable to this reaction under near neutral conditions, with good to excellent yields.
- Cheng, Xionglve,Jiang, Gangzhong,Li, Xingxing,Tao, Suyan,Wan, Xiaobing,Zhao, Yanwei,Zheng, Yonggao
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supporting information
p. 2713 - 2718
(2021/06/25)
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- SULFONAMIDE DERIVATIVES AND USES THEREOF
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The present disclosure relates to compounds of Formula (I) or (II): and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
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Paragraph 0859
(2020/12/30)
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- AMINO-BENZOISOTHIAZOLE AND AMINO-BENZOISOTHIADIAZOLE AMIDE COMPOUNDS
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Provided herein are amino-benzoisothiazole and benzoisothiadiazole amide compounds. In particular, provided herein are compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds provided herein are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, retinal diseases such as acute macular degeneration (AMD) and diabetic macular edema (DME), diseases and conditions characterized by inflammatory processes, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. Also provided are compositions (e.g., pharmaceutical compositions) comprising the compounds provided herein.
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Paragraph 00220
(2019/10/04)
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- HETEROCYCLIC COMPOUNDS
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The present invention relates to compounds of the general formula (1) wherein the variables are defined as given in the description and claims. The invention further relates to uses of and to, processes and intermediates related to compounds of the general formula (I), wherein Q is wherein the substituents of I, Ia and Ib are as defined in description and claims.
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Page/Page column 75
(2018/07/29)
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- EZH2 Inhibitors
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The present invention relates to compounds that inhibit EZH2 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
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Paragraph 0405; 0407; 0408
(2018/11/02)
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- Interface engineering of hybrid perovskite solar cells with poly(3-thiophene acetic acid) under ambient conditions
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The properties of methyl ammonium lead iodide (MAPbI3) perovskite solar cells with poly(3-thiophene acetic acid) (P3TAA) as a hole transporting material (HTM) and a dense layer of ZnO nanoparticle film as an electron transporting material (ETM) are described using the conventional ZnO (n)/perovskite (i)/P3TAA (p) (n-i-p) architecture. The FT-IR spectra of a MAPbI3/P3TAA mixture indicate a shift of the N-H stretching and the abolition of the N-H bending peak indicating the interaction between the components. UV-Vis spectra of the mixture exhibit a large red shift of the π-π? transition peak of the conjugated chain arising from the interaction causing an increase of the conjugation length. The cross-sectional SEM image of the device shows the sequence of the individual layers of ZnO, MAPbI3, P3TAA and Ag, respectively. The current density (J)-voltage (V) curves obtained upon illumination with a light of 100 mW cm-2 indicate the average PCE to be 7.38 ± 0.59% under ambient conditions. The IPCE values of these cells reach about 63% across a broad range of wavelength (300-800 nm). The HOMO and the LUMO of P3TAA are measured using cyclic voltammetry and the optical band gap and the relative energy level of the components explain the operation of photocurrent in the cell. For comparison purposes a device using poly(3-hexyl thiophene) (P3HT) as the HTM is fabricated under similar conditions and it exhibits a lower PCE (5.85 ± 0.51%) than that of the P3TAA based device. The longevity of the P3TAA based cell is also found to be better than that of the P3HT based cell for storing in air. The UV-Vis and impedance spectral results clearly explain the above results, signifying the influence of the interface on the performance of hybrid solar cells.
- Shit, Arnab,Nandi, Arun K.
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p. 10182 - 10190
(2016/05/19)
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- INTEGRATED ZWITTERIONIC CONJUGATED POLYMERS FOR BIOELECTRONICS, BIOSENSING, REGENERATIVE MEDICINE, AND ENERGY APPLICATIONS
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The present invention is directed to a versatile and high performance zwitterionic CP platform, which integrates all desired functions into one material. This zwitterionic CP consists of the conducting backbone and multifunctional zwitterionic side chains. Non-conducting zwitterionic materials gain electronic conductivity through the conducting backbone and CPs obtain excellent biocompatibility, sensitivity to environmental stimuli and controllable antifouling properties via multifunctional zwitterionic side chains. Unique properties from two distinct materials (conducting materials and zwitterionic materials) are integrated into one material without sacrificing any properties. This platform can potentially be adapted for a range of applications (e.g. bioelectronics, tissue engineering, wound healing, robotic prostheses, biofuel cell, etc.), which all require high performance conducting materials with excellent antifouling/biocompatibility at complex biointerfaces. This conducting material platform will significantly advance the development of conducting polymers in the field of biomedicine and biotechnology.
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(2015/04/28)
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- Acetylcholinesterase-induced fluorescence turn-off of an oligothiophene-grafted quartz surface sensitive to myristoylcholine
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Conjugated polyelectrolytes (CPEs) have recently emerged as label-free materials for biosensing due to their intrinsic ability to transduce an amplified optical signal in response to interactions with different analytes. Herein, the conformational change of an anionic oligothiophene is exploited to generate a unique fluorescent response upon interaction with myristoylcholine (MyrCh). The variations observed in spectroscopic signals are explained in terms of a synergistic combination of hydrophobic and electrostatic forces involving the oligothiophene chains and MyrCh molecules, inducing the disassembling of oligothiophene chains. The enzyme acetylcholinesterase (AChE) is able to reverse this effect by catalyzing the hydrolysis of MyrCh; hence, its enzymatic activity can be monitored through the variation of fluorescence emission of the system. The oligothiophene sensing probe retains its conformational sensitivity with regard to the AChE-mediated cleavage of MyrCh upon immobilization onto a quartz substrate, which is accomplished by a "grafting onto" approach based on click chemistry. These results are encouraging for the further development of such a label-free system towards the fabrication of sensing devices that would incorporate CPEs and would be potentially useful for the specific detection of a wide range of bioanalytes. This journal is
- Grisci,Mróz,Giovanella,Pagano,Porzio,Ragona,Samperi,Tomaselli,Galeotti,Destri
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supporting information
p. 4892 - 4903
(2015/06/25)
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- Rhodium-catalyzed oxygenative addition to terminal alkynes for the synthesis of esters, amides, and carboxylic acids
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A gem of a couple: The title reaction of terminal alkynes with O and Nnucleophiles proceeds in the presence of [Rh(cod)Cl}2], P(4-FC 6H4)3, and 4-picoline N-oxide. Alcohols, amines, and water add to the terminal alkynes to give esters, amides, and carboxylic acids, respectively. The reaction involves formation of a rhodium vinylidene, oxidation to a ketene by oxygen transfer, and nucleophilic addition.
- Kim, Insu,Lee, Chulbom
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supporting information
p. 10023 - 10026
(2013/10/01)
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- NOVEL COMPOUNDS AND THEIR USE IN THERAPY
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The present invention relates to novel chemical compounds formula (I) (C)n-B-(A)m-B-(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five-and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (-CO-), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.
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Page/Page column 31
(2013/03/26)
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- NOVEL THIOPHENE COMPOUNDS AND METHOD FOR IN VIVO IMAGING
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The present invention relates to novel labelled compounds of formula (I) (C)n-B-(A)m-B-(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group ( -CO- ), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1, for use in imaging amyloid deposits and aggregated protein in living patients. The invention further relates to imaging methods using labelled or unlabelled compounds of formual I and the use of unlabelled compounds in such methods.
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Page/Page column 38
(2013/03/26)
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- The structural basis for optimal performance of oligothiophene-based fluorescent amyloid ligands: Conformational flexibility is essential for spectral assignment of a diversity of protein aggregates
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Protein misfolding diseases are characterized by deposition of protein aggregates, and optical ligands for molecular characterization of these disease-associated structures are important for understanding their potential role in the pathogenesis of the disease. Luminescent conjugated oligothiophenes (LCOs) have proven useful for optical identification of a broader subset of disease-associated protein aggregates than conventional ligands, such as thioflavin T and Congo red. Herein, the molecular requirements for achieving LCOs able to detect nonthioflavinophilic Aβ aggregates or non-congophilic prion aggregates, as well as spectrally discriminate Aβ and tau aggregates, were investigated. An anionic pentameric LCO was subjected to chemical engineering by: 1) replacing thiophene units with selenophene or phenylene moieties, or 2) alternating the anionic substituents along the thiophene backbone. In addition, two asymmetric tetrameric ligands were generated. Overall, the results from this study identified conformational freedom and extended conjugation of the conjugated backbone as crucial determinants for obtaining superior thiophene-based optical ligands for sensitive detection and spectral assignment of disease-associated protein aggregates. Copyright
- Klingstedt, Therese,Shirani, Hamid,Aslund, K. O. Andreas,Cairns, Nigel J.,Sigurdson, Christina J.,Goedert, Michel,Nilsson, K. Peter R.
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supporting information
p. 10179 - 10192
(2013/09/02)
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- Synthesis of a library of oligothiophenes and their utilization as fluorescent ligands for spectral assignment of protein aggregates
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Molecular probes for selective identification of protein aggregates are important to advance our understanding of the molecular pathogenesis underlying protein aggregation diseases. Here we report the chemical design of a library of anionic luminescent conjugated oligothiophenes (LCOs), which can be utilized as ligands for detection of protein aggregates. Certain molecular requirements were shown to be necessary for detecting (i) early non-thioflavinophilic protein assemblies of Aβ1-42 and insulin preceding the formation of amyloid fibrils and (ii) for obtaining distinct spectral signatures of the two main pathological hallmarks observed in human Alzheimer's diease brain tissue (Aβ plaques and neurofibrillary tangles). Our findings suggest that a superior anionic LCO-based ligand should have a backbone consisting of five to seven thiophene units and carboxyl groups extending the conjugated thiophene backbone. Such LCOs will be highly useful for studying the underlying molecular events of protein aggregation diseases and could also be utilized for the development of novel diagnostic tools for these diseases. The Royal Society of Chemistry 2011.
- Klingstedt, Therese,Aslund, Andreas,Simon, Rozalyn A.,Johansson, Leif B. G.,Mason, Jeffrey J.,Nystroem, Sofie,Hammarstroem, Per,Nilsson, K. Peter R.
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experimental part
p. 8356 - 8370
(2012/04/23)
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- Synthesis of novel furo-, thieno-, and pyrroloazepines
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The synthesis of novel furo-, thieno-, and pyrroloazepine compounds, using the oxidative radical alkylation of three five-membered heterocyclic 3-acetic acid derivatives, is described. The bicyclic systems were obtained, via a small number of steps, directly from commercially available materials. Georg Thieme Verlag Stuttgart New York.
- Villarreal, Carlos,Martinez, Roberto
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experimental part
p. 3346 - 3352
(2010/11/17)
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- BETA- AND GAMMA-AMINO-ISOQUINOLINE AMIDE COMPOUNDS AND SUBSTITUTED BENZAMIDE COMPOUNDS
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Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
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Page/Page column 13-14
(2010/02/17)
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- SMALL-MOLECULE BOTULINUM TOXIN INHIBITORS
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Small-molecule inhibitors of Botulinum toxin, including BoNTA, BoNTD and BoNTE are provided, as well as methods of using the inhibitors.
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- Synthesis of selective SRPK-1 inhibitors: Novel tricyclic quinoxaline derivatives
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SR protein-specific kinase-1 (SRPK-1) has been identified as a validated target for hepatitis B virus (HBV). A series of novel tricyclic quinoxaline derivatives was designed and synthesised as potential kinase inhibitory antiviral agents and was found to be active and selective for SRPK-1 kinase. Most of these novel compounds have drug-like properties according to experimentally determined Log P and Log S values.
- Szekelyhidi, Zsolt,Pato, Janos,Waczek, Frigyes,Banhegyi, Peter,Hegymegi-Barakonyi, Balint,Eros, Daniel,Meszaros, Gyoergy,Hollosy, Ferenc,Hafenbradl, Doris,Obert, Sabine,Klebl, Bert,Keri, Gyoergy,Orfi, Laszlo
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p. 3241 - 3246
(2007/10/03)
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- Catalytic asymmetric cyclopropanation of heteroaryldiazoacetates
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Rh2(S-DOSP)4-catalyzed decomposition of heteroaryldiazoacetates in the presence of styrene results in highly diastereoselective and enantioselective cyclopropanations. Heteroaryldiazoacetates containing both electron-rich and electron-deficient heterocycles, such as thiophene, furan, pyridine, indole, oxazole, isoxazole, and benzoxazole, are effective in this chemistry. These studies broaden the range of diazo compounds containing both electron-withdrawing and electron-donating groups, which undergo highly diastereoselective cyclopropanations.
- Davies,Townsend
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p. 6595 - 6603
(2007/10/03)
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- Synthesis and antifungal activity evaluation of 3-hetaryl-2,5-dihydrofuran-2-ones. An unusual fragmentation of the oxazole ring via 2,3-selenoxide shift
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In continuing the studies on the synthesis and evaluation of antifungal activity of the analogues of (-)incrustoporine, the replacement of the phenyl moiety at C3 of the furanone ring with a hetaryl substituent was considered. Thus, a series of 5-alkyl-3-hetaryl-2,5-dihydrofuran-2-ones with the thienyl, furyl and thiazolyl moieties attached to C3 was synthesized, and the compounds subjected to antifungal activity screening. In the preparation of compounds containing the oxazolyl fragment, the [2,3]-sigmatropic rearrangement led to the fragmentation of the oxazole ring, resulting in the formation of 3-(1-benzamido-2-oxoethylidene)-5-methyltetrahydrofuran-2-one. Somewhat surprisingly, the antifungal efficiency of the derivatives was lower in comparison with analogues containing a substituted phenyl at C3.
- Kunes, Jiri,Balsanek, Vojtech,Pour, Milan,Buchta, Vladimir
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p. 1809 - 1830
(2007/10/03)
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- Condensed compounds, their production and use
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This invention provides new condensed furan compounds which exhibit excellent 2,3-oxidosqualene cyclase inhibition and high-density lipoprotein-cholesterol elevating activities. This invention also provides a therapeutic and prophylactic agent for hyperlipidemia, hypercholesterolemia and atherosclerosis.
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- Nickel-catalysed electrochemical coupling of 2- and 3-bromothiophene with alkyl and alkenyl halides
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2- or 3-bromothiophene are efficiently coupled with activated alkyl chlorides (α-chloroesters, α-chloroketones, α-chloronitriles), benzyl chloride or vinyl halides, in a one step electrochemical reaction, using the sacrificial anode process and catalysis by NiBr2-2,2'-bipyridine (bipy).
- Durandetti, Muriel,Perichon, Jacques,Nedelec, Jean-Yves
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p. 8683 - 8686
(2007/10/03)
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- Thiophene Systems. 10. The Synthesis and Chemistry of some Thienopyridinols
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Substituted thieno-, thieno- and thienopyridinols have not been described despite the fact that a few descriptions of the parent ring systems have appeared in the literature.As a part of our ongoing program to investigate the synthesis of thiophene derivatives with potential biological activity, we became interested in the preparation of the various thienopyridinols.Syntheses of the title compounds 2a, 3 and 25 were achieved starting from thiophene-3-acetic acid and 3-acetylthiophene.The two isomeric systems 2a and 3 were reacted with electrophiles to give products substituted at the position α to the hydroxy group on the pyridine ring (the 4- and 6- positions, respectively).Lack of stability of 25 precluded studies on this system.Compound 2a, 3 and 25 reacted with acetic anhydride to give O-acetyl derivatives while reaction of the anion of 2a and 3 with methyl iodide gave mixtures of O- and N-methylation.The N-methylated products are the novel thienopyridones 45 and 47.
- Press, Jeffery B.,McNally, James J.
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p. 1571 - 1581
(2007/10/02)
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- Acid-catalyzed rearrangement of cyclobutanols. A novel rearrangement
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The acid-catalysed dehydration-rearrangement reaction of α-thienyl cyclobutanols 3 and 4 resulted in the formation of tetrahydronaphthothiophenes 5a and 6a.The rearrangement to the linearly fused PAH system instead of the expected angularly fused system reflects α-scission of the cyclobutyl ring.A mechanism based on deuterium labelling studies is propesed to account for the product formation.
- Lee-Ruff, E.,Ablenas, Fred J.
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p. 1663 - 1667
(2007/10/02)
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- DEHALOGENATION OF ETHYL 2,5-DICHLORO-3-THIENYLGLYOXYLATE IN THE PRESENCE OF SUPPORTED PALADIUM COMPLEXES
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The dependence of the rate and selectivity of the catalytic hydrodehaligenation of ethyl 2,5-dichloro-3-thienylglyoxylate over immobilized palladium complexes on the nature of the solvent and HCl has been investigated.Hydrogenation of the C=O group also occurs.Reductive dechlorination of methyl and ethyl 2,5-dichloro-3-thienylacetates occurs selectively, at a slower rate than in the case of the 3-thienylglyoxylate.
- Gurovets, A. S.,Sharf, V. Z.,Taits, S. Z.,Vol'kenshtein, Yu. B.,Fabrichnyi, B. P.
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p. 1331 - 1336
(2007/10/02)
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- Process for the preparation of thiophenes
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A process for the preparation of 3-substituted thiophenes which involves cyclization of a novel intermediate, avoids the use of previously employed expensive starting materials. The thiophenes are useful for the preparation of penicillins and cephalosporins. The process is for the preparation of a thiophene of formula (I): STR1 where R1 represents a carboxylic acid group, or an ester or amide thereof or a nitrile group; R2 represents a group suitable for use as an α-substituent in the side-chain of a penicillin or cephalosporin; which comprises treating a compound of formula (II): STR2 wherein X represents halogen or optionally functionalized hydroxyl, Y represents halogen, hydroxyl, or alkoxy; with a source of nucleophilic sulphur under basic conditions.
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- Thiophene derivatives and process for preparation thereof
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Commercially advantageous processes for preparing thienylacetic acid, furylacetic acid or alkyl esters of these. Novel thiophene or furan derivatives that can be used as starting materials for preparing the above compounds. Processes for preparing these starting materials are also provided.
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