534-97-4Relevant articles and documents
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Randall
, p. 173,177 (1969)
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Amin,El-Sayed
, p. 39,44 (1973)
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Mia,Phillips
, p. 100 (1965)
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Kiang et al.
, p. 1035,1036 (1968)
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Plant mucilages. XI. Isolation and characterization of a mucosa polysaccharide, 'paniculatan', from the barks of Hydrangea paniculata
Tomoda,Satoh
, p. 230 - 234 (1976)
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A fine-tuned lipophilicity/hydrophilicity ratio governs antibacterial potency and selectivity of bifurcated halogen bond-forming nbtis
?akelj, Simon,Anderluh, Marko,Hrast, Martina,Kokot, Maja,Kolari?, Anja,Minovski, Nikola,Trontelj, Jurij,Weiss, Matja?,Zdovc, Irena
, (2021/07/31)
Herein, we report the design of a focused library of novel bacterial topoisomerase inhibitors (NBTIs) based on innovative mainly monocyclic right-hand side fragments active against DNA gyrase and Topo IV. They exhibit a very potent and wide range of antibacterial activity, even against some of the most concerning hard-to-treat pathogens for which new antibacterials are urgently needed, as reported by the WHO and CDC. NBTIs enzyme activity and whole cell potency seems to depend on the fine-tuned lipophilicity/hydrophilicity ratio that governs the permeability of those compounds through the bacterial membranes. Lipophilicity of NBTIs is apparently optimal for passing through the membrane of Gram-positive bacteria, but the higher, although not excessive lipophilicity and suitable hydrophilicity seems to determine the passage through Gram-negative bacterial membranes. However, due to the considerable hERG inhibition, which is still at least two orders of magnitude away from MICs, continued optimization is required to realize their full potential.
1-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in?vitro and inflammatory response in?vivo
Gonzaga, Daniel Tadeu Gomes,Ferreira, Leonardo Braga Gomes,Moreira Maramaldo Costa, Thadeu Estevam,von Ranke, Natalia Lidmar,Anastácio Furtado Pacheco, Paulo,Sposito Sim?es, Ana Paula,Arruda, Juliana Carvalho,Dantas, Luiza Pereira,de Freitas, Hércules Rezende,de Melo Reis, Ricardo Augusto,Penido, Carmen,Bello, Murilo Lamim,Castro, Helena Carla,Rodrigues, Carlos Rangel,Ferreira, Vitor Francisco,Faria, Robson Xavier,da Silva, Fernando de Carvalho
, p. 698 - 717 (2017/09/01)
Fifty-one 1,2,3-triazole derivatives were synthesized and evaluated with respect to P2X7 receptor (P2X7R) activity and its associated pore. These triazoles were screened in vitro for dye uptake assay and its cytotoxicity against mammalian cell types. Seven 1,2,3-triazole derivatives (5e, 6e, 8h, 9d, 9i, 11, and 12) potently blocked P2X7 receptor pore formation in vitro (J774.G8 cells and peritoneal macrophages). All blockers displayed IC50 value inferior to 500 nM, and they have low toxicity in either cell types. These seven selected triazoles inhibited P2X7R mediated interleukin-1 (IL-1β) release. In particular, compound 9d was the most potent P2X7R blocker. Additionally, in mouse acute models of inflammatory responses induced by ATP or carrageenan administration in the paw, compound 9d promoted a potent blocking response. Similarly, 9d also reduced mouse LPS-induced pleurisy cellularity. In silico predictions indicate this molecule appropriate to develop an anti-inflammatory agent when it was compared to commercial analogs. Electrophysiological studies suggest a competitive mechanism of action of 9d to block P2X7 receptor. Molecular docking was performed on the ATP binding site in order to observe the preferential interaction pose, indicating that binding mode of the 9d is by interacting its 1,2,3-triazole and ether moiety with positively charged residues and with its chlorobenzene moiety orientated toward the apolar end of the ATP binding site which are mainly composed by the Ile170, Trp167 and Leu309 residues from α subunit. These results highlight 9d derivative as a drug candidate with potential therapeutic application based on P2X7 receptor blockade.
Determination of glyceraldehyde formed in glucose degradation and glycation
Usui, Teruyuki,Yoshino, Miku,Watanabe, Hirohito,Hayase, Fumitaka
, p. 2162 - 2168 (2008/09/18)
Glyceraldehyde (GLA) was determined in glucose degradation and glycation. GLA was detected as a decahydroacridine-1,8-dione derivative on reversed phase HPLC using cyclohexane-1,3-dione derivatizing reagent. The glucose-derived GLA level was higher than the glycation-derived GLA level, because GLA was converted to intermediates and advanced glycation end products (AGE) in glycation. GLA was also generated from 3-deoxyglucosone and glucosone as intermediates of glucose degradation and glycation. This study suggests that glyceraldehyde is generated by hyperglycemia in diabetes, and that it is also formed in medicines such as peritoneal dialysis solution.