135062-06-5Relevant academic research and scientific papers
Guanylthiourea derivatives as potential antimalarial agents: Synthesis, in?vivo and molecular modelling studies
Bhagat, Shweta,Arfeen, Minhajul,Adane, Legesse,Singh, Savita,Singh, Prati Pal,Chakraborti, Asit K.,Bharatam, Prasad V.
, p. 339 - 348 (2017)
Guanylthiourea (GTU) derivatives were identified as possible anti-malarial agents, recently, using in?vitro studies on Plasmodium falciparum. This article gives an account of the in?vivo anti-malarial activity of GTU derivatives against experimental rodent malaria. A total of 20 synthesized GTU derivatives were evaluated for in?vivo antimalarial activity, out of which six showed encouraging results; one compound appeared to have curative potential. Molecular docking and molecular dynamics analysis were carried out to understand the molecular level interactions.
Cascade energy transfer and tunable emission from nanosheet hybrids: Locating acceptor molecules through chiral doping
Goudappagouda,Wakchaure, Vivek Chandrakant,Ranjeesh, Kayaramkodath Chandran,Abhai, Chalona Antony Ralph,Babu, Sukumaran Santhosh
, p. 7072 - 7075 (2017)
Light harvesting donor-acceptor assemblies are indispensable to efficiently tap photons. In an attempt to improve the light harvesting efficiency of an acceptor doped assembly, we design and synthesize a donor-acceptor-donor triad which exhibits an except
Intracellular Ruthenium-Promoted (2+2+2) Cycloadditions
Miguel-ávila, Joan,Tomás-Gamasa, María,Mascare?as, José L.
supporting information, p. 17628 - 17633 (2020/08/14)
Metal-mediated intracellular reactions are becoming invaluable tools in chemical and cell biology, and hold promise for strongly impacting the field of biomedicine. Most of the reactions reported so far involve either uncaging or redox processes. Demonstrated here for the first time is the viability of performing multicomponent alkyne cycloaromatizations inside live mammalian cells using ruthenium catalysts. Both fully intramolecular and intermolecular cycloadditions of diynes with alkynes are feasible, the latter providing an intracellular synthesis of appealing anthraquinones. The power of the approach is further demonstrated by generating anthraquinone AIEgens (AIE=aggregation induced emission) that otherwise do not go inside cells, and by modifying the intracellular distribution of the products by simply varying the type of ruthenium complex.
ANTIMICROBIAL MATERIALS AND METHODS
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Page/Page column 20; 48, (2013/03/26)
The invention provides methods and materials for decontamination of surfaces and fabrics, such as non-woven fabrics, that are contaminated with infestations of microorganisms such as bacteria. Biocidal oligomers having conjugated oligo-(aryl/heteroaryl et
Evaluation of novel aryloxyalkyl derivatives of imidazole and 1,2,4-triazole as heme oxygenase-1 (HO-1) inhibitors and their antitumor properties
Salerno, Loredana,Pittalà, Valeria,Romeo, Giuseppe,Modica, Maria N.,Siracusa, Maria A.,Di Giacomo, Claudia,Acquaviva, Rosaria,Barbagallo, Ignazio,Tibullo, Daniele,Sorrenti, Valeria
, p. 5145 - 5153 (2013/09/02)
A novel series of aryloxyalkyl derivatives of imidazole and 1,2,4-triazole, 17-31, was designed and synthesized as inhibitors of heme oxygenase-1 (HO-1) and heme oxygenase-2 (HO-2). Some of these compounds were found to be good inhibitors of HO-1, in particular those carrying an imidazole moiety as azolyl group and a 3-bromo or 4-iodophenyl as aryl moiety. The most potent compounds 6 and 30 were selected and studied for their antitumor properties in a model of LAMA-84 R cell line overexpressing HO-1 and resistant to imatinib mesylate (IM), a tyrosine-kinase inhibitor used in the treatment of multiple types of cancer, most notably Philadelphia Chromosome positive (Ph+) Chronic Myelogenous Leukemia (CML). Results show that both 6 and 30 sensitized LAMA-84 R cell line to antitumor properties of IM.
STRUCTURE, SYNTHESIS, AND APPLICATIONS FOR OLIGO PHENYLENE ETHYNYLENES (OPES)
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Page/Page column 3; 13, (2012/02/02)
The present disclosure provides novel oligo phenylene ethynylene (OPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various OPEs show antibacterial, antiviral and antifungal activity.
A new disubstituted polyacetylene bearing pyridine moieties: Convenient synthesis and sensitive chemosensor toward sulfide anion with high selectivity
Zhang, Liang,Lou, Xiaoding,Yu, Yun,Qin, Jingui,Li, Zhen
experimental part, p. 5186 - 5193 (2012/04/17)
To develop sensitive and selective S2- chemosensors, a new disubstituted polyacetylene (P2) bearing pyridine moieties in the side chains was prepared conveniently through a postfunctional method, the strong green fluorescence of which could be completely quenched by Cu2+ ions at the concentration as low as 2.0 × 10-6 mol/L in diluted solutions. Based on the displacement strategy, by utilizing the much higher stability constant of the complex of S2- and Cu2+, the quenched fluorescence of the solution of P2 by Cu2+ ions could recover upon the addition of trace S2- anions, with the detection limit down to 5.0 × 10-7 mol/L. Moreover, no interference were observed from other anions, including SO32-, HSO 3-, SO42-, ClO4 -, I-, Br-, Cl-, F-, IO3-, HPO42-, PO4 3-, C2O42-, S2O 32-, CO32-, AcO-, CN -, and P2O74-, making P2 a novel, sensitive, and selective sulfide probe.
NOVEL PHENYL-ISOXAZOL-3-OL DERIVATIVE
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Page/Page column 49, (2009/09/26)
The present invention relates to a compound represented by formula (I), which has a GPR120 agonist action and thus is useful for treatment of diabetes mellitus or hyperlipidemia, or a pharmaceutically acceptable salt thereof. In the formula, (AA) represents a phenyl or the like, which may be substituted with a lower alkoxy group or the like; (BB) represents a divalent group or the like, derived by removal of two hydrogen atoms from a benzene which may be substituted with a halogen atom or the like; X represents a spacer having a main chain composed of 1-8 carbon atoms wherein 1-3 carbon atoms in the main chain may be substituted with an oxygen atom or the like; and Y represents a hydrogen atom or the like.
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity
Lewis, Timothy A.,Young, Michelle A.,Arrington, Mark P.,Bayless, Lynn,Cai, Xiong,Collart, Philippe,Eckman, Joseph B.,Ellis, James L.,Ene, Doina G.,Libertine, Lyn,Nicolas, Jean-Marie,Scannell, Ralph T.,Wels, Bruce F.,Wenberg, Karen,Wypij, Donna M.
, p. 5591 - 5594 (2007/10/03)
Three different histaminergic H1 scaffolds were attached by various linkers to a single 5-LO scaffold. Both activities were observed in vitro. Pharmacokinetic properties of the compounds were evaluated and both a cetirizine-based compound and a
Synthesis of fluorine and iodine analogues of clorgyline and selective inhibition of monoamine oxidase A
Ohmomo,Hirata,Murakami,Magata,Tanaka,Yokoyama
, p. 1038 - 1040 (2007/10/02)
A series of fluorine and iodine analogues of clorgyline was synthesized and evaluated for inhibitory potency and selectivity toward monoamine oxidase A (MAO-A). Among them, N-[3-(2,4-dichloro-6-iodophenoxy)propyl]-N-methyl-2-propynylamine (3d), N-[3-(4-ch
