20376-36-7Relevant academic research and scientific papers
A rhodamine derivative as selective fluorescent and colorimetric chemosensor for mercury (II) in buffer solution, test strips and living cells
Wang, Meng,Yan, Fan-Yong,Zou, Yu,Yang, Ning,Chen, Li,Chen, Li-Gong
, p. 216 - 223 (2014)
In this paper, we reported a new rhodamine derivative bearing 2,4-dichloroquinazoline as a selective fluorescent chemosensor for Hg 2+. The ring-opening process of spirolactam enabled the large fluorescent enhancement and colorimetric change by Hg2+ induced configuration transformation of the rhodamine. Moreover, the fluorescence changes of the chemosensor were dramatically specific for Hg2+ in the presence of other metal ions, which could meet the selective requirements for practical application. Under optimized experimental conditions, the linear response range covered the concentration range of Hg2+ from 0 to 1.0 × 10-6 M, and the limit of detection was calculated to be 2.7 × 10-8 M. In addition, the probe was also successfully applied to the determination of Hg2+ in water samples, test strips and living cells.
Design, synthesis, biological evaluation, and molecular docking study on triazine based derivatives as anti-inflammatory agents
Alvani, Mohsen,Asadi, Parvin,Hajhashemi, Valiollah,Khodarahmi, Ghadamali,Rostami, Mahboubeh
, (2021/07/01)
In an attempt to develop new anti-inflammatory agents, design, synthesis, pharmacological activities, and docking study of two groups of triazine-based derivatives were reported. Nine compounds (5a-5d and 10a-10e) consisting of triazine, vanillin, and phenylpyrazole were synthesized through the pharmacophore hybridization method. After confirmation of the structure of the synthesized compounds using spectroscopic methods (FT-IR, and NMR spectral data), their anti-inflammatory activity was evaluated using carrageenan-induced paw edema model in male Wistar rats (200–220 g) administered intraperitoneally at doses of 100 and 200 mg/kg. A group of rats received indomethacin (10 mg/kg) as the standard drug. Among compounds 5a to 5d, only compounds 5c and 5d showed a significant anti-inflammatory effect (p 0.01). Also compound 10a at a dose of (200 mg/kg) and compounds 10b, 10c, 10d and 10e at both doses showed significant anti-inflammatory activity and this effect for 10a (200 mg/kg) and both doses of 10b and 10e was comparable with indomethacin. While indomethacin reduced paw edema by 90%, 10b as the most potent tested compound reduced edema by 93%. The synthesized compounds were docked into the binding sites of both cyclooxygenase-1- and 2- isoenzymes (COX-1 and COX-2) to explore their binding mode and possible interactions of these ligands.
Design, Synthesis and Pharmacological Evaluation of Novel Hsp90N-terminal Inhibitors Without Induction of Heat Shock Response
Liu, Peng,Chen, Xiangling,Zhu, Jianming,Li, Bo,Chen, Zhaoqiang,Wang, Guimin,Sun, Haiguo,Xu, Zhijian,Zhao, Zhixin,Zhou, Chen,Xie, Chengying,Lou, Liguang,Zhu, Weiliang
, p. 344 - 353 (2019/04/04)
Heat shock protein 90 (Hsp90) is a potential oncogenic target. However, Hsp90 inhibitors in clinical trial induce heat shock response, resulting in drug resistance and inefficiency. In this study, we designed and synthesized a series of novel triazine der
Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice
Singh, Palwinder,Kaur, Sukhmeet,Kumari, Priya,Kaur, Baljit,Kaur, Manpreet,Singh, Gurjit,Bhatti, Rajbir,Bhatti, Manpreet
, p. 7929 - 7941 (2018/09/06)
Here, we report analgesic and anti-inflammatory activity of a series of compounds obtained by appending 4-aminophenylmorpholin-3-one and acyclic, cyclic, or heterocyclic moieties on 1,3,5-triazine. The structures of compounds 4b and 6b are optimized for the best inhibition of COX-2 with IC50 values of 0.06 and 0.08 μM, respectively, and selectivity over COX-1 of 166 and >125, respectively. At the dose of 5 mg kg-1, these compounds significantly reduced acetic acid induced writhings, and their ED50 values were found to be 2.2 and 1.9 mg kg-1, respectively. Besides the cell-based and animal-based experiments showing the modes of action of these compounds targeting COX-2, the interaction behavior of 4b with COX-2 was also characterized, with physicochemical experiments including ITC, NMR, UV-vis, and molecular-modeling studies. Characteristically, these compounds interact with R120, Y355, and W385, the residues responsible for holding the substrate and mediating the process of electron transfer during the metabolic phase of the enzyme.
Synthesis and in vitro antibacterial screening of some new 2,4,6-trisubstituted-1,3,5-triazine derivatives
Singh, Ravi Bhushan,Das, Nirupam,Jana, Srabanti,Das, Aparoop
experimental part, p. 316 - 321 (2012/06/18)
With an objective to evaluate the antibacterial activity of triazine derivatives, a series of 2,4,6-trisubstituted-1,3,5-triazine were synthesized and characterized by FTIR, 1H-NMR, 13C-NMR, mass spectroscopy and elemental analysis. The minimum inhibitory concentration (MIC) of the compounds that displayed favourable zone of inhibition was determined by broth microdilution method. Derivatives with morpholinyl substituent (4a and 4i) demonstrated good in vitro activities against Gram-positive organisms, whereas two of the compound bearing a diethylamino side chain exhibited moderate (4e) to broad spectrum (4j) activity comparable to streptomycin. The promising activity of the latter maybe attributed to the substitution of electron releasing group at para position of phenyl rings.
Triaminotriazine DNA helicase inhibitors with antibacterial activity
McKay, Geoffrey A.,Reddy, Ranga,Arhin, Francis,Belley, Adam,Lehoux, Dario,Moeck, Greg,Sarmiento, Ingrid,Parr, Thomas R.,Gros, Philippe,Pelletier, Jerry,Far, Adel Rafai
, p. 1286 - 1290 (2007/10/03)
Screening of a chemical library in a DNA helicase assay involving the Pseudomonas aeruginosa DnaB helicase provided a triaminotriazine inhibitor with good antibacterial activity but associated cytotoxicity toward mammalian cells. Synthesis of analogs provided a few inhibitors that retained antibacterial activity and demonstrated a significant reduction in cytotoxicity. The impact of serum and initial investigations toward a mode of action highlight several features of this class of compounds as antibacterials.
Structure-activity relationships of novel antibacterial translation inhibitors: 3,5-Diamino-piperidinyl triazines
Zhou, Yuefen,Sun, Zhongxiang,Froelich, Jamie M.,Hermann, Thomas,Wall, Daniel
, p. 5451 - 5456 (2007/10/03)
Structure-activity relationships of the 3,5-diamino-piperidinyl triazine series, a novel class of bacterial translation inhibitors, are described. Optimization was focused on the triazine C-4 position in which aromatic substituents that contained electron-withdrawing groups led to potent inhibitors. The initial lack of antibacterial activity was correlated with poor cellular penetration. Whole cell antibacterial activity was achieved by linking additional aromatic moieties at the triazine C-4 position.
A triazine core for a new class of Sharpless asymmetric dihydroxylation ligands
McNamara, Catherine Anne,King, Frank,Bradley, Mark
, p. 8527 - 8529 (2007/10/03)
Sharpless asymmetric dihydroxylation ligands were synthesized using a triazine spacer group in two, high yielding steps and gave good enantioselectivities in the asymmetric dihydroxylation of alkenes. Sharpless asymmetric dihydroxylation ligands were synthesized using a triazine spacer group in two, high yielding steps from cheap, readily available starting materials. The ligands, gave good enantioselectivities in the asymmetric dihydroxylation of alkenes and may provide a very economic alternative to current systems.
