2231-57-4Relevant articles and documents
Rare-earth (Eu3+, Tb3+) hybrids through amide bridge: Chemically bonded self-assembly and photophysical properties
Liu, Jinliang,Yan, Bing
, p. 580 - 587 (2010)
This work focuses on the construction of a series of chemically bonded rare-earth/inorganic/organic hybrid materials (TCH-Si-Ln, TCH-Si-Ln-Phen and TCH-Si-Ln-Bipy: Phen = 1,10-phenanthroline, Bipy = 2,2′-bipyridyl) using TCH-Si as an organic bridge molecule that can both coordinate to rare-earth ions (Eu3+ and Tb3+) and form an inorganic Si-O-Si network with tetraethoxysilane (TEOS) after cohydrolysis and copolycondensation through a sol-gel process. All of these hybrid materials exhibit homogeneous microstructures and morphologies, suggesting the occurrence of self-assembly of the inorganic network and organic chain. Measurements of the photoluminescent properties of these materials show that the ternary europium systems present stronger luminescent intensities than the binary hybrids, indicating that the introduction of the second ligands can sensitize the luminescence emission of the europium hybrid systems. However, in the terbium systems, this phenomenon was not observed.
Three-input-three-output logic operations based on absorption and fluorescence dual-mode from a thiourea compound
Wang, Lianlian,Li, Bin,Zhang, Liming,Luo, Yongshi
, p. 459 - 465 (2013)
A simple organic molecule of 2-naphthol-1-aldehyde-conjugated thiourea (denoted as receptor 1) is designed and prepared. Absorption and fluorescence spectra response profiles of receptor 1 with different ionic inputs vary significantly in a DMSO-H2O solution (V/V = 9 : 1) through modulating intramolecular charge transfer (ICT) processes. In particular, the changes of the dual-modal spectra when anions, such as F-, AcO- or H2PO4-, are introduced in such an aqueous solution indicate that receptor 1 could be tolerant to H2O at least to some extent in recognizing anions. On the basis of the above results, binary logic operations (OR, NOR and INHIBIT) and their multiply-logic functions with different combinations have been achieved at the molecular level by changing different chemical inputs. The output signals can be encoded as absorption and fluorescence dual-mode, depending on the choice of 2-naphthol as the chromophore and fluorophore core.
Design, synthesis and docking studies of a novel ciprofloxacin analogue as an antimicrobial agent
Jubie,Kalirajan,Yadav, Pavankumar
, p. 980 - 987 (2012)
The carboxylic acid group of ciprofloxacin was modified and amino mercapto triazole was substituted. The compound was confirmed by physical parameters (solubility, melting point), chromatographic methods (TLC) and consistent with its IR & 1HNMR spectra. The synthesized analogue was screened for antibacterial activity against one gram positive & two gram negative species. The compound exhibited good antibacterial effect towards gram negative species when compared to the standard ciprofloxacin. At the same time the analogue was retaining antibacterial activity towards gram positive species when compared to standard ciprofloxacin. The molecular docking studies showed a good correlation between their antibacterial activity and autodock binding free energy.
4-amino-1,2,4-triazole-3-thione as a promising scaffold for the inhibition of serine and metallo-β-lactamases
Linciano, Pasquale,Gianquinto, Eleonora,Montanari, Martina,Maso, Lorenzo,Bellio, Pierangelo,Cebrián-Sastre, Esmeralda,Celenza, Giuseppe,Blázquez, Jesús,Cendron, Laura,Spyrakis, Francesca,Tondi, Donatella
, (2020)
The emergence of bacteria that co-express serine-and metallo-carbapenemases is a threat to the efficacy of the available β-lactam antibiotic armamentarium. The 4-amino-1,2,4-triazole-3-thione scaffold has been selected as the starting chemical moiety in the design of a small library of β-Lactamase inhibitors (BLIs) with extended activity profiles. The synthesised compounds have been validated in vitro against class A serine β?Lactamase (SBLs) KPC-2 and class B1 metallo β?Lactamases (MBLs) VIM-1 and IMP-1. Of the synthesised derivatives, four compounds showed cross-class micromolar inhibition potency and therefore underwent in silico analyses to elucidate their binding mode within the catalytic pockets of serine-and metallo-BLs. Moreover, several members of the synthesised library have been evaluated, in combination with meropenem (MEM), against clinical strains that overexpress BLs for their ability to synergise carbapenems.
Design, synthesis and biological evaluation of pleuromutilin-Schiff base hybrids as potent anti-MRSA agents in vitro and in vivo
Li, Bo,Zhang, Zhe,Zhang, Jian-Feng,Liu, Jie,Zuo, Xiang-Yi,Chen, Fang,Zhang, Guang-Yu,Fang, Han-Qing,Jin, Zhen,Tang, You-Zhi
, (2021/06/22)
A series of pleuromutilin derivatives with 1,2,4-triazole-3-substituted Schiff base structure were designed and synthesized under mild conditions. The in vitro antibacterial activities of the synthesized derivatives against 4 strains of Staphylococcus aureus (MRSA ATCC 43300, S.aureus ATCC 29213, S.aureus 144 and S.aureus AD3) and 1 strain of E. coli (ATCC 25922) were evaluated by the broth dilution method. Among these derivatives, compound 60 exhibited superior in vitro antibacterial effect against MRSA (MIC = 0.25 μg/mL) than tiamulin (MIC = 0.5 μg/mL), and compound 60 (?2.28 log10 CFU/mL) also displayed superior in vivo antibacterial efficacy than tiamulin (?1.40 log10 CFU/mL) in reducing MRSA load in the mouse thigh infection model. The time-kill study and the post-antibiotic effect study indicated that compound 60 showed a faster bactericidal kinetic and longer PAE time (exposure to 2 × MIC and 4 × MIC for 2 h, the PAE was 4.06 and 4.27 h) against MRSA compared with tiamulin (exposure to 2 × MIC and 4 × MIC for 2 h, the PAE was 1.72 and 2.14 h). Meanwhile, most of these compounds had no significant inhibitory effect on RAW 264.7 cells and HepG2 cells at the concentration of 4 μg/mL. Additionally, the development of resistance study showed that MRSA did not easily develop resistance against compound 60 compared with tiamulin after induction for 8 passages.
Pleuromutilin derivative with 1,2,4-triazole Schiff base as well as preparation and application of pleuromutilin derivative
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Paragraph 0102-0103, (2020/10/04)
The invention belongs to the field of medicinal chemistry, and particularly relates to a pleuromutilin derivative with 1,2,4-triazole Schiff base as well as preparation and application of the pleuromutilin derivative. The pleuromutilin derivative with 1,2,4-triazole Schiff base is a compound represented by a formula 2 or a pharmaceutically acceptable salt thereof, and a solvate, an enantiomer, a diastereoisomer, a tautomer or a mixture of the solvate, the enantiomer, the diastereoisomer and the tautomer of the compound of formula 2 or the pharmaceutically acceptable salt thereof, the compoundnot only has good in-vitro antibacterial activity, but also has the advantage of low preparation cost compared with valnemulin and retapamulin, so that the compound is particularly suitable for beingused as a novel antibacterial drug for preventing and treating human or animal bacterial infectious diseases, particularly infectious diseases caused by drug-resistant staphylococcus aureus.
