- Hybrid 4-Aminoquinoline-1,3,5-triazine Derivatives: Design, Synthesis, Characterization, and Antibacterial Evaluation
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A series of novel 4-aminoquinoline 1,3,5-triazine derivatives were synthesized and characterized by FTIR, 1H-NMR, 13C-NMR, MS, and elemental analysis. The antibacterial activities of synthesized compounds were tested against three Gram-positive bacteria, namely Bacillus subtilis (NCIM-2063), Bacillus cereus (NCIM-2156), and Staphylococcus aureus (NCIM-2079), and four Gram-negative bacteria, namely Proteus vulgaris (NCIM-2027), Proteus mirabilis (NCIM-2241), Escherichia coli (NCIM-2065), and Pseudomonas aeruginosa (NCIM-2036), using ciprofloxacin as reference standard drug. Results showed compound 9a and 9e as potent antibacterial agents against all bacterial strains except Bacillus cereus (NCIM-2156).
- Pathak,Thakur,Bhat,Singh
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- Sulfonamide-1,3,5-triazine-thiazoles: Discovery of a novel class of antidiabetic agents: Via inhibition of DPP-4
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Dipeptidyl peptidase-4 (DPP-4) inhibitors are a novel class of antidiabetic drugs used for treating type 2 diabetes mellitus. In the present study, a novel hybrid sulphonamide-1,3,5-triazine-thiazole derivatives were synthesized and characterized by 1H-NMR, 13C-NMR, FT-IR, mass spectroscopy and elemental analysis. The result showed that among the tested compounds, 8c was found to be a more potent inhibitor of DPP-4 (2.32 nM) than the alogliptin standard. Moreover, molecular docking results showed that ligand 8c was efficiently docked into the active site of the catalytic triad of Ser630, Asp708 and His740, encompassing both the S1 and S2 pocket with a CDOCKER interaction energy of 57.80. The in vitro results were further substantiated by in vivo blood glucose lowering effects in experimental subjects. The results of the investigation showed that compound 8c exhibited concentration-dependent improvement of glucose tolerance in ICR after oral administration. It has been also found that compound 8c (30 mg kg-1) showed a reduction in the area under the curve from 0 to 120 min [(AUC) 0-120 min] to 37.46%, which was found to be approximately similar to the hypoglycemic profile of alogliptin (standard). The activity of compound 8c was also investigated in STZ-induced diabetic rats where it showed a dose-dependent decrease in blood glucose levels together with an improvement in insulin levels probably via inhibition of DPP-4. The effect of compound 8c was also investigated on the lipid profile and antioxidant enzyme system.
- Gao, Hai-De,Liu, Peng,Yang, Yang,Gao, Fang
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- BICYCLIC COMPOUND AND USE THEREOF FOR INHIBITING SUV39H2
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The present invention directs to a compound represented by formula (I).
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Page/Page column 330; 331
(2017/08/01)
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- Halogen-free expansion type flame retardant containing thiotriazinone phosphoramidate and preparation method thereof
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The invention relates to a halogen-free expansion type flame retardant containing thiotriazinone phosphoramidate and a preparation method thereof. Tricyanogen chloride, piperazine, organic amine, ammonia water and phosphoryl chloride serve as main raw materials, the compound is prepared through replacing and condensation reactions, and the advantages that the raw materials are easy to obtain and production is stable are achieved. The obtained compound containing P-N piperazine-riazine-phosphate ester structural units combines a carbon source, a gas source and an acid source into one molecular structure. The flame retardant has good water-resistant characteristic and can serve as flame retardant of most high-polymer materials, and good application prospects are achieved.
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Paragraph 0042; 0043; 0044; 0045
(2016/10/31)
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