- Synthesis of the end-functionalized polymethyl methacrylate incorporated with an asymmetrical porphyrin group via atom transfer radical polymerization and investigation on the third-order nonlinear optical properties
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A novel asymmetrical zinc(II) porphyrin (ZnPor-Br) was synthesized as the initiator for the atom transfer radical polymerization (ATRP). Using CuBr/2,2′-dipyridyl as the catalyst system, the ATRP of polymethyl methacrylate (PMMA) was carried out to afford
- Qiu, Nannan,Liu, Dajun,Han, Shuangli,He, Xingquan,Cui, Guihua,Duan, Qian
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Read Online
- Formulation of antimicrobial tobramycin loaded PLGA nanoparticles via complexation with AOT
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Tobramycin is a potent antimicrobial aminoglycoside and its effective delivery by encapsulation within nanoparticle carriers could increase its activity against infections through a combination of sustained release and enhanced uptake. Effective antimicro
- Hill, Marcus,Cunningham, Richard N.,Hathout, Rania M.,Johnston, Christopher,Hardy, John G.,Migaud, Marie E.
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Read Online
- Thermoresponsive dynamic covalent single-chain polymer nanoparticles reversibly transform into a hydrogel
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To gel and back: Polymer nanoparticles can be reversibly transformed into a chemically cross-linked hydrogel. This transformation is triggered by the application of heat, which causes the polymer chains to aggregate, and the dynamic nature of the covalent cross-linking serves to reorganize the polymer chains into a hydrogel network. Copyright
- Whitaker, Daniel E.,Mahon, Clare S.,Fulton, David A.
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Read Online
- Protective effects of two novel nitronyl nitroxide radicals on heart failure induced by hypobaric hypoxia
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Aims: Hypobaric hypoxia (HH), linked to oxidative stress, impairs cardiac function. We synthesized a novel nitronyl nitroxide radical, an HPN derivative (HEPN) and investigated the protective effects of HEPN and HPN against HH-induced heart injury in mice and the underlying mechanisms of action. Main methods: Mice were administered with HPN (200 mg/kg) or HEPN (200 mg/kg) 30 min before exposed to HH. The cardiac function was measured. Serum AST, CK, LDH and cTnI were estimated. Heart tissue oxidase activity, SOD, CAT, GSH-Px, ROS and MDA were estimated. ATP content, Na+/K+-ATPase and Ca2+/Mg2+-ATPase activity was measured. The expression of HIF-1, VEGF, Nrf2, HO-1, Bax, Bcl-2, Caspase-3 was estimated. Key findings: Results showed that pretreatment with HEPN or HPN led to a dramatic decrease in the activity of biochemical markers AST, CK, LDH and cTnI in murine serum. They increased the activity of SOD, CAT and GSH-Px and reduced the level of ROS and MDA in the hearts of mice. HEPN and HPN could increase the expression of Nrf2 and OH-1. They could maintain the ATPase activity. The Bax and Caspase-3 expression as well as the ratio of Bax/Bcl-2 were significantly downregulated and the Bcl-2 expression was upregulated by HPN or HEPN compared to the HH group. They may attenuate the HH-induced oxidant stress via free radical scavenging activity. Significance: The present study showed that the nitronyl nitroxide radical HEPN and HPN may be potential therapeutic agents for treatment of HH-induced cardiac dysfunction.
- Jia, Zhengping,Jing, Linlin,Lan, Ting,Ma, Huiping,Shao, Jin,Sun, Wei,Wang, Haibo
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Read Online
- Chemoselective and ligand-free aerobic oxidation of benzylic alcohols to carbonyl compounds using alumina-supported mesoporous nickel nanoparticle as an efficient recyclable heterogeneous catalyst
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An economically efficient and operationally simple ligand-free protocol for the chemoselective oxidation of benzylic alcohols to carbonyl compounds has been developed using alumina-supported nickel nanoparticles as a stable recyclable heterogeneous catalyst along with potassium tert-butoxide in the presence of aerial oxygen as an eco-friendly oxidant. The aliphatic alcohols remained unaffected under the present condition. Excellent chemoselectivity has also been demonstrated through intermolecular and intramolecular competition experiments. This protocol accommodates a diverse range of substituents with the tolerance of various sensitive moieties during the reaction. The catalyst could be recovered by filtration and reused consecutively without any significant loss in the catalytic activity. Moreover, the heterogeneity of the catalyst has also been established by the “hot filtration method (Sheldon's test)”.
- Das, Asit Kumar,Nandy, Sneha,Bhar, Sanjay
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- Semirotaxanes and unsymmetrical rotaxanes from substituted benzylammonium salts and dibenzo-24-crown-8
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Three new hydroxyl-functionalized secondary benzyl ammonium salts were synthesized and complexed with dibenzo-24-crown-8. Three [2]semirotaxanes and then their two [2]rotaxanes each with two different stoppers were prepared successfully by reactions of th
- Niu, Zhenbin,Fletcher, Amy L.,Slebodnick, Carla,Gibson, Harry W.
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- Light-induced energy transfer followed by electron transfer in axially co-ordinated benzothiazole tethered zinc porphyrin-fullero[C60/C70]pyrrolidine triads
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Benzothiazole (BTZ)-zinc porphyrin (ZnP) dyads, Dyad-1 and Dyad-2 connected together with two different spacers, ester and ethoxy esters, were synthesized and light induced energy and electron transfer events were investigated. Within these dyads, due to
- Chitta, Raghu,Badgurjar, Deepak,Reddy, Govind,Jain, Kanika,Karla, Vijendar Reddy,Boligorla, Anjaiah,Giribabu, Lingamallu
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p. 469 - 483
(2021/04/05)
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- Four component Passerini polymerization of bulky monomers under high shear flow
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We introduce a four component Passerini polymerization utilizing sterically bulky isocyanide monomers. Under typical Passerini conditions, bulky isocyanides do not react within standard Passerini reaction timescales (hours). We overcome this challenge via the unique physiochemical conditions present in a vortex fluidic device, reducing the reaction time to 2 h on average. Under these high-shear thin-film conditions, bulky isocyanides are readily incorporated into the multicomponent polymerization without the need of high-pressure or temperature. Finally, we demonstrate that the four component approach using functional cyclic anhydrides allows for post-polymerization modification.
- Barner-Kowollik, Christopher,Bui, Aaron H.,Raston, Colin L.,Truong, Vinh X.,Tuten, Bryan T.,Wiedbrauk, Sandra
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supporting information
p. 8328 - 8331
(2021/08/25)
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- Arylpyrazole compound and application thereof
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The invention discloses an arylpyrazole compound. The arylpyrazole compound has a structure shown in the description. The arylpyrazole compound has good selective PDE4 inhibition activity and weak PDE4D inhibition effect, and can show more excellent pharm
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Paragraph 0060; 0062-0064
(2020/06/20)
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- Auxin fluorescent dye, and preparation method and application thereof
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The invention discloses an auxin fluorescent dye, and a preparation method and application thereof. The auxin fluorescent probe has a structural formula shown in the specification. The preparation method of the auxin fluorescent probe comprises the follow
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Paragraph 0065-0068
(2020/11/02)
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- Fe3O4@SiO2@Im-bisethylFc [HC2O4] as a novel recyclable heterogeneous nanocatalyst for synthesis of bis-coumarin derivatives
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Nanomagnetic bisethylferrocene-containing ionic liquid supported on silica-coated iron oxide (Fe3O4@SiO2@Im-bisethylFc [HC2O4]) as a novel catalyst was designed and synthesized. The described catalyst
- Teimuri-Mofrad, Reza,Tahmasebi, Shabnam,Payami, Elmira
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- Potassium ion probe, preparation method and applications thereof
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The invention relates to a potassium ion probe, a preparation method and applications thereof, wherein the potassium ion probe has high selectivity to potassium ions, can emit green fluorescence and detect K concentration, contains hydroxyl so as to be
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Paragraph 0089-0094
(2019/11/21)
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- Bisferrocene-containing ionic liquid supported on silica coated Fe3O4: A novel nanomagnetic catalyst for the synthesis of dihydropyrano[2,3-c]coumarin derivatives
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Nanomagnetic bisferrocene-containing ionic liquid supported on silica coated Fe3O4 (Fe3O4@SiO2@imidazol-bisFc[HCO3]) as a novel heterogeneous catalyst was synthesized and the structure and
- Teimuri-Mofrad, Reza,Esmati, Somayeh,Tahmasebi, Shabnam,Gholamhosseini-Nazari, Mahdi
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- Fluorescence probe for detecting zinc ions, and preparation method and application thereof
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The invention relates to a fluorescence probe for detecting zinc ions, and a preparation method and an application thereof. The fluorescence probe is a high-fluorescence dimethylpyrrole BODIPY. The fluorescence probe is chemically named as 8-[4-(1-oxocarb
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Paragraph 0036; 0037; 0038; 0039; 0046-0049; 0055-0058
(2017/10/07)
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- Carbon nitride assisted chemoselective C-H bond photo-oxidation of alkylphenolethoxylates in water medium
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The unprecedented ability of g-C3N4 to chemoselectively photo-oxidise the methyl group of 2-(4-methylphenoxy)ethanol instead of the easily oxidised oxyethanol fragment has been demonstrated. When g-C3N4 is treat
- Ilkaeva,Krivtsov,Bartashevich,Khainakov,García,Díaz,Ordó?ez
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supporting information
p. 4299 - 4304
(2017/09/29)
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- Ovicidal and insecticidal activities of pyriproxyfen derivatives with an oxime ester group
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Based on the structural framework of a pyriproxyfen metabolite, nineteen oxime ester derivatives were synthesized via reaction of the carboxylic acids with 4-(2-(2-pyridinyloxy) ethoxy)benzaldehyde oxime. The corresponding structures were comprehensively
- Sun, Guo-Shao,Xu, Xin,Jin, Shu-Hui,Lin, Le,Zhang, Jian-Jun
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- Compound and application of compound to treating colon cancer
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The invention discloses a compound and application of the compound to treating the colon cancer. The structural formula of the compound is shown in the formula I, wherein R1, R2, R3 and R4 in the formula I are respectively independently chosen from alkyl groups and alkoxy groups, the number of hydrogen atoms, halogen, nitro and carbon atoms in the alkyl group is 1-6, the number of carbon atoms in the alkoxy group is 1-6, R5 is chosen from nitro and -NR6R7, wherein R6 and R7 are respectively independently the hydrogen atom or CH2Ar, the Ar represents a phenyl group or an aryl group, the para-position of the aryl group is substituted by R8, the aryl group is a phenyl group, the R8 is an alkoxy group or the following shown groups, and the number of halogen, hydroxyl and carbon atoms in the R8 is 1-6. The compound also has an obvious effect on inhibiting a tumor sphere from a cancer patient with the colon cancer. In addition, the compound also has an obvious effect on inhibiting the migration and the moving ability of a colon cancer cell line. A novel medicine for treating the colon cancer is expected to be developed on the basis of the compound.
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Paragraph 0174-0177
(2017/11/04)
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- π-Conjugate Fluorophore-Tagged and Enzyme-Responsive l -Amino Acid Polymer Nanocarrier and Their Color-Tunable Intracellular FRET Probe in Cancer Cells
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The present investigation accounts one of the first example of enzyme-responsive and π-conjugate-tagged l-amino acid amphiphilic polymer and their fluorescence resonance energy transfer (FRET) probes for color-tunable intracellular bioimaging in cancer ce
- Saxena, Sonashree,Jayakannan, Manickam
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p. 2594 - 2609
(2017/08/18)
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- Pyridine-ethylbenzene-ether oxime esterPyrene ethylbenzene oxime-ethers esters compound, and preparation method and application thereof
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The invention discloses a pyridine-ethylbenzene-ether oxime esterpyrene ethylbenzene oxime-ethers esters compound, and a preparation method and application thereof, belonging to the technical field of agricultural chemistry. The preparation method compris
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Paragraph 0031; 0032; 0033
(2016/10/09)
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- Synthesis and investigation of novel benzimidazole derivatives as antifungal agents
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The rise and emergence of resistance to antifungal drugs by diverse pathogenic fungal strains have resulted in an increase in demand for new antifungal agents. Various heterocyclic scaffolds with different mechanisms of action against fungi have been investigated in the past. Herein, we report the synthesis and antifungal activities of 18 alkylated mono-, bis-, and trisbenzimidazole derivatives, their toxicities against mammalian cells, as well as their ability to induce reactive oxygen species (ROS) in yeast cells. Many of our bisbenzimidazole compounds exhibited moderate to excellent antifungal activities against all tested fungal strains, with MIC values ranging from 15.6 to 0.975?μg/mL. The fungal activity profiles of our bisbenzimidazoles were found to be dependent on alkyl chain length. Our most potent compounds were found to display equal or superior antifungal activity when compared to the currently used agents amphotericin B, fluconazole, itraconazole, posaconazole, and voriconazole against many of the strains tested.
- Chandrika, Nishad Thamban,Shrestha, Sanjib K.,Ngo, Huy X.,Garneau-Tsodikova, Sylvie
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supporting information
p. 3680 - 3686
(2016/07/20)
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- TREATMENT OF DISEASES BY EPIGENETIC REGULATION
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The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.
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Paragraph 0452; 0453
(2013/11/05)
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- Methoxy-poly(ethylene glycol)-block-poly(ε-caprolactone) bearing pendant aldehyde groups as pH-responsive drug delivery carrier
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A biodegradable amphiphilic block copolymer of methoxy poly(ethylene glycol)-block-poly(ε-caprolactone) bearing pendant aldehyde groups was synthesised by a combination of ring-opening polymerisation and thio-bromo 'click' chemistry. The free aldehyde gro
- Ma, Gejun,Li, Deshan,Wang, Ji,Zhang, Xuefei,Tang, Haoyu
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p. 1576 - 1583
(2014/01/23)
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- A dual fluorinated and iodinated radiotracer for PET and SPECT imaging of β-amyloid plaques in the brain
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We report a fluorinated and iodinated radiotracer as a probe for PET/SPECT to detect of β-amyloid (Aβ) plaques in the brain of patients with Alzheimer's disease (AD). We successfully designed and synthesized the fluorinated and iodinated aurone derivative
- Watanabe, Hiroyuki,Ono, Masahiro,Kimura, Hiroyuki,Kagawa, Shinya,Nishii, Ryuichi,Fuchigami, Takeshi,Haratake, Mamoru,Nakayama, Morio,Saji, Hideo
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supporting information; experimental part
p. 6519 - 6522
(2011/12/04)
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- Photoactivated 1,3-dipolar cycloaddition for the rapid preparation of 18F labelled radiotracers
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An 18F-labelled 2,5-diaryl tetrazole reagent has been prepared and reacted with substituted alkene dipolarophiles through a photoactivated 1,3-dipolar cycloaddition reaction. The radiobioconjugation reaction furnished the desired product in 5 m
- Thonon, David,Goukens, Eve,Kaisin, Geoffroy,Paris, Jér?me,Flagothier, Jessica,Luxen, André
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experimental part
p. 5572 - 5576
(2011/08/09)
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- Mpg-C3N4-catalyzed selective oxidation of alcohols using O2 and visible light
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Mesoporous carbon nitride (mpg-C3N4) polymer can function as a metal-free photocatalyst to activate O2 for the selective oxidation of benzyl alcohols with visible light, avoiding the cost, toxicity, and purification problems associated with corresponding transition-metal systems. By combining the surface basicity and semiconductor functions of mpg-C3N4, the photocatalytic system can realize a high catalytic selectivity to generate benzaldehyde. The metal-free photocatalytic system also selectively converts other alcohol substrates to their corresponding aldehydes/ketones, demonstrating a potential pathway of accessing traditional mild radical chemistry with nitroxyl radicals.
- Su, Fangzheng,Mathew, Smitha C.,Lipner, Grzegorz,Fu, Xianzhi,Antonietti, Markus,Blechert, Siegfried,Wang, Xinchen
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supporting information; experimental part
p. 16299 - 16301
(2011/02/22)
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- Synthesis and biological evaluation of novel 4-hydroxybenzaldehyde derivatives as tyrosinase inhibitors
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A series of novel 4-hydroxybenzaldehyde derivatives were synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were investigated. Most of target compounds had more potent inhibitory activities than the parent compound 4-hydroxybenzaldehyde (IC50 = 1.22 mM). Interestingly, compound 3c bearing a dimethoxyl phosphate was found to be the most potent inhibitor with IC50 value of 0.059 mM. The inhibition kinetics analyzed by Lineweaver-Burk plots revealed that compound 3c was a non-competitive inhibitor (KI = 0.0368 mM). In particular, compound 3c showed no side effects at dose of 1600 mg/kg in mice. These results suggested that such compounds might be served as lead compounds for further designing new potential tyrosinase inhibitors.
- Yi, Wei,Cao, Rihui,Peng, Wenlie,Wen, Huan,Yan, Qin,Zhou, Binhua,Ma, Lin,Song, Huacan
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experimental part
p. 639 - 646
(2010/04/02)
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- NOVEL ANTI-INFLAMMATORY AGENTS
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Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.
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Page/Page column 87-88
(2010/11/05)
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- Rational design and synthesis of 4-O-substituted phenylmethylenethiosemicarbazones as novel tyrosinase inhibitors
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In continuing our program aimed to search for tyrosinase inhibitors, a series of novel 4-O-substituted phenylmethylenethiosemicarbazones were rational designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were also evaluated. A fair number of compounds were found to have significant tyrosinase inhibitiory activity. Particularly, the IC50 values of compounds 3a-g, 3j and 3s were of the same magnitude as tropolone, one of the best tyrosinase inhibitors known so far. Furthermore, the structure-activity relationships of these compounds were also investigated. All these data suggested that these molecules might be utilized for the development of new candidate for the treatment of dermatological disorders, and further development of such compounds may be of interest.
- Yi, Wei,Cao, Rihui,Chen, Zhiyong,Yu, Liang,Wen, Huan,Yan, Qin,Ma, Lin,Song, Huacan
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scheme or table
p. 752 - 754
(2010/07/15)
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- Reactive thermoresponsive copolymer scaffolds
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Thermoresponsive copolymer scaffolds containing reactive aldehyde functions were prepared and a selection of organic residues conjugated to these copolymer scaffolds through oxime/hydrazone formation. The conjugation of hydrophobic residues affords copoly
- Murray, Benjamin S.,Jackson, Alexander W.,Mahon, Clare S.,Fulton, David A.
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supporting information; experimental part
p. 8651 - 8653
(2011/01/03)
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- Inhibitory effects of 5-benzylidene barbiturate derivatives on mushroom tyrosinase and their antibacterial activities
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A series of novel 5-benzylidene barbiturate and thiobarbiturate derivatives were synthesized and evaluated as tyrosinase inhibitors and antibacterial agents. The results demonstrated that some compounds had more potent inhibitory activities than the parent compound 4-hydroxybenzaldehyde (IC50 = 1.22 mM). Particularly, compounds 1a and 2a were found to be the most potent inhibitors with IC50 value of 13.98 μM and 14.49 μM, respectively. The inhibition mechanism study revealed that these compounds were irreversible inhibitors. The circular dichroism spectra indicated that these compounds induced conformational changes of mushroom tyrosinase upon binding. In addition, these compounds exhibited selectively antibacterial activity against Staphylococcus aureus. All these results suggested that further development of such compounds may be of interest.
- Yan, Qin,Cao, Rihui,Yi, Wei,Chen, Zhiyong,Wen, Huan,Ma, Lin,Song, Huacan
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experimental part
p. 4235 - 4243
(2009/12/24)
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- A tunable photosensor
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A pyrene-modified β-cyclodextrin (pyrenecyclodextrin)-decorated single-walled carbon nanotube (SWNT) field-effect transistor (FET) device was fabricated, which can serve as a tunable photosensor to sense a fluorescent adamantyl-modified Ru complex (ADA-Ru
- Zhao, Yan-Li,Hu, Liangbing,Grüner, George,Stoddart, J. Fraser
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scheme or table
p. 16996 - 17003
(2009/04/13)
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- NOVEL ANTIDIABETIC COMPOUNDS
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The present invention provides novel compounds of the general formula (I), wherein the symbols are same as described in specification, their pharmaceutically acceptable salts, their tautomeric forms, their stereoisomers, pharmaceutical compositions containing them, to process and intermediates for the preparation of the above said compounds, having the utility of these compounds in medicine and to methods for their therapeutic use, and their use in the treatment of diabetes and related diseases.
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Page/Page column 92
(2010/11/29)
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- INDOLINONE DERIVATIVES AS RECEPTOR TYROSINE KINASE IHIBITORS
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Novel derivatives of compound (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one and the use thereof for the preparation of medicaments for the treatment of tumors in which the tyrosine kinase activity proteins Met, PDGF-R, FGF-R1
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Page/Page column 31-32
(2008/06/13)
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- Indolinone derivatives
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Novel derivatives of compound (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one and the use thereof for the preparation of medicaments for the treatment of tumors in which the tyrosine kinase activity proteins Met, PDGF-R, FGF-R1
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Page/Page column 15
(2008/06/13)
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- MESO-SUBSTITUTED PORPHYRINS
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Meso-substituted porphyrins of general formula (I) suitable for the use as photosensitising agents, in particular in photodynamic therapy, are herein described.
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- Chemical modification of coumarin dimer and HIV-1 integrase inhibitory activity
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A systematic series of chemically modified coumarin dimmers has been synthesized and tested for their inhibitory activity against HIV-1 integrase. We observed that modified coumarin dimmers containing hydrophobic moiety on the linker display potent inhibi
- Mao, Pili Chih-Min,Mouscadet, Jean-Francois,Leh, Herve,Auclair, Christian,Hsu, Ling-Yih
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p. 1634 - 1637
(2007/10/03)
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- 1,2-dithiolane derivatives
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This invention provides new thiazolindinedione derivatives and new arylacetic acid derivatives. These compounds are useful for the treatment of cardiovascular diseases, certain endocrine diseases, certain inflammatory diseases, certain neoplastic (maligna
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- Synthesis of two calix[4]arenes in 1,3-alternate conformation containing hard and soft ion binding sites
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It is reported the synthesis of ligands 6 and 8 combining one calix[4]arene unit in the 1,3-alternate conformation and crown ether and aza crown ether elements. Preliminary complexations are given.
- Aeungmaitrepirom, Wanlapa,Asfari, Zouhair,Vicens, Jacques
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p. 1907 - 1910
(2007/10/03)
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- Nitrostyrene derivatives of adenosine 5'-glutarates modified with an alkyl spacer and their inhibitory activity on epidermal growth factor receptor protein tyrosine kinase
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β-Nitrostyrene derivatives of adenosine 5'-glutarates are potent and selective bisubstrate-type inhibitors of the epidermal growth factor receptor protein tyrosine kinase (EGF-R PTK). In an attempt to improve the inhibitory activity, this type of compounds was modified with alkyl spacers of varying length between the nitrostyrene and the glutaryl units. The spacers consisted of 1, 3, 4, and 5 atoms to give compounds of the benzyl, oxyethyl, oxypropyl, and oxybutyl series, respectively (Schemes 1 and 2). Adenosine 5'-esters were prepared in the benzyl and oxypropyl series only. Compared to the compounds in the parent series without spacer (IC50 = 0.7-12 μM), most of the modified compounds inhibited the EGF-R PTK only marginally or were inactive (IC50 ≥ 100 μM). The only exceptions were the free acids 19 and 20 with IC50 values of ca. 5 μM. It is noteworthy that esterification of these two hydrogen glutarates with either MeOH or adenosine yielded inactive compounds, which is in contrast to the corresponding substances without spacers.
- Peterli,Hubmann,Sequin,Mett,Traxler
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