423156-68-7Relevant academic research and scientific papers
3-methyl pyridino-[1,2-a] pyrimidone derivative containing 1-((4-benzyl-substituted)oxygroup) and application
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Paragraph 0134; 0136, (2019/04/30)
The invention discloses a 3-methyl pyridino-[1,2-a] pyrimidone derivative containing 1-((4-benzyl-substituted)oxygroup) and application. The general formula of the derivative is shown in the description, wherein R1 is a methoxyl group or an oxyethyl group or halogen; R2 is hydroxyl or isobutyl or ethyl or propyl or chloroethyl or 2-methoxyl group benzyl or 2-methoxyl group benzy or 2-fluorine benzyl or 2-cyanogroup benzyl chloride or 4-cyanogroup benzyl2-methyl benzyl chloride or 3-methyl benzyl chloride or 4-methyl benzyl chloride. According to the derivative, the rice bacterial leaf blight and citrus canker can be prevented and treated. The general formula is shown in the description.
First Discovery of Novel Pyrido[1,2- a]pyrimidinone Mesoionic Compounds as Antibacterial Agents
Liu, Dengyue,Zhang, Jian,Zhao, Lei,He, Wengjing,Liu, Zhengjun,Gan, Xiuhai,Song, Baoan
, (2019/10/21)
Plant bacterial diseases cause tremendous decreases in crop yield and quality, and there is a lack of highly effective and low-risk antibacterial agents. A series of novel pyrido[1,2-a]pyrimidinone mesoionic compounds containing vanillin moieties were synthesized, and the application of these mesoionic compounds as plant antibacterial agents was reported here for the first time. The bioassay results revealed that the mesoionic compounds had good antibacterial activity. Of these compounds, compound 11 showed excellent in vitro activity against Xanthomonas oryzae pv. oryzae, with an EC50 value of 1.1 μg/mL, which was substantially better than that of bismerthiazol (92.7 μg/mL) and thiodiazole copper (105.4 μg/mL). Moreover, greenhouse condition trials indicated that the protective and curative activities of compound 11 against rice bacterial leaf blight were 75.12 and 72.04%, respectively, which were better than those of bismerthiazol (62.24 and 50.83%, respectively) and thiodiazole copper (53.35 and 65.04%, respectively). These results provide a basis for the application of mesoionic vanillin moieties as new antibacterial agents.
Biological evaluation and in silico molecular docking study of a new series of thiazol-2-yl-hydrazone conglomerates
Bhat, Mahima,Gurubasavaraja Swamy,Poojary, Boja,Revanasiddappa,Vijay Kumar,Kumar, Vasantha
, p. 2779 - 2805 (2018/02/19)
A new series of hybridized thiazol-2-yl-hydrazone derivatives having diverse substituents were designed, synthesized, and screened for their anti-inflammatory property by a carrageenan-induced paw edema method. The compounds 11a, 11b, 11c, 11d, 11e, 11g, 11m and 11p revealed significant inhibition when compared to Diclofenac sodium. Subsequently, two highly potent compounds (11d and 11e) were evaluated for their cytotoxic effect on the tumor cell line. The binding interactions of thiazol-2-yl-hydrazones with the cyclooxygenase-2 (COX-2) protein (PDB: 3LN1) displayed effective interactions with Arg-120, Tyr-385 and Tyr-355 amino acids, the main criteria of the COX-2 inhibitor. In addition, all the compounds showed moderate to good in vitro antibacterial activity. Most active benzyloxy derivatives were also tested to understand the radical scavenging efficacy by the 2,2-diphenyl-1-picrylhydrazyl method. Graphical Abstract: [Figure not available: see fulltext.].
Vanillin-derived antiproliferative compounds influence Plk1 activity
Carrasco-Gomez, Roberto,Keppner-Witter, Sarah,Hieke, Martina,Lange, Lisa,Schneider, Gisbert,Schubert-Zsilavecz, Manfred,Proschak, Ewgenij,Sp?nkuch, Birgit
supporting information, p. 5063 - 5069 (2014/12/11)
We synthesized a series of vanillin-derived compounds and analyzed them in HeLa cells for their effects on the proliferation of cancer cells. The molecules are derivatives of the lead compound SBE13, a potent inhibitor of the inactive conformation of huma
SUBSTITUDED BENZYLOXY-PHENYLMETHYLUREA DERIVATIVES
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Page/Page column 22, (2010/11/28)
The present invention relates to novel substituted benzyloxy-phenylmethylurea derivatives, processes for their preparation, and their use in medicaments, especially for the prophylaxis and treatment of diseases associated with Cold Menthol Receptor 1 (CMR
SUBSTITUTED 4-BENZYLOXY-PHENYLMETHYLAMIDE DERIVATIVES AS COLD MENTHOL RECEPTOR-1 (CMR-1) ANTAGONISTS FOR THE TREATMENT OF UROLOGICAL DISORDER
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Page/Page column 20, (2008/06/13)
The present invention relates to novel substituted benzyloxy-phenylmethylamide derivatives of formula (I), processes for their preparation, and their use in medicaments, especially for the prophylaxis and treatment of diseases associated with Cold Menthol
N-acyl-N'-benzyl-alkylendiamino drivatives
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Page/Page column 12, (2008/06/13)
This invention is related to compounds and use of N-Acyl-N'-benzylalkylendiamino derivatives of the following general formula I???whereinAis a straight or branched C2-C8 alkyl chain;Xis a methylene, oxygen, sulphur or a NR7/sup
