- N-(2-guanidino-ethylimino)-morpholine antigen based on thiotriazinone structure restrictiveness, antibody and application
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The present invention discloses a N-(2-guanidino-ethylimino)-morpholine hapten based on thiotriazinone structure restrictiveness, an artificial antigen, an antibody and an application. The structure of the N-(2-guanidino-ethylimino)-morpholine hapten is represented by a formula I shown in the description, wherein R is -H and -CH3. The N-(2-guanidino-ethylimino)-morpholine artificial antigen and antibody are prepared base on the hapten, and the artificial antigen and antibody have high detection efficiency and simple operation to N-(2-guanidino-ethylimino)-morpholine, and can be used in enzyme-linked immunosorbent assay rapid detection of the N-(2-guanidino-ethylimino)-morpholine; and the antigen and the antibody have a simple synthetic process, lower costs, and good application prospects.
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Paragraph 0049; 0054; 0055
(2018/06/04)
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- Synthesis and in Vitro AMPK Activation of Cycloalkyl/Alkarylbiguanides with Robust in Vivo Antihyperglycemic Action
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This work describes the design, synthesis in one step, and the in vitro, in vivo, and in silico antidiabetic evaluation of a series of ten alicyclic and aromatic (alkyl +aryl: alkaryl)biguanides, analogues of metformin and phenformin. The design was conceived using isosteric replacement, chain-ring transformation, and lower and higher homologation strategies. All compounds were obtained as crystals and their structure was confirmed on the basis of their spectral data (NMR and mass spectra), and their purity was ascertained by microanalysis. Compounds were in vitro evaluated as activators of AMP-Activated Protein Kinase (AMPK). The results indicated that compounds 4, 5, and 6 showed similar or even better effect compared to metformin. Docking analysis was performed with regulatory subunit γ of AMPK, showing several interactions with nucleotide binding pocket. The in vivo evaluation of compounds 4-6 at a single dose of 50 mg/kg was performed in a murine experimental model of diabetes. The results showed an important and robust decrease of plasmatic glucose levels (-40%). Compound 6 was selected for an oral glucose tolerance test, showing an antihyperglycemic effect similar to metformin. The in vivo results indicated that compounds 4-6 may be effective in treating experimental T2DM.
- Gutierrez-Lara, Erika,Martínez-Conde, Carlos,Rosales-Ortega, Edgar,Ramírez-Espinosa, Juan José,Rivera-Leyva, Julio C.,Centurión, David,Carvajal, Karla,Ortega-Cuellar, Daniel,Estrada-Soto, Samuel,Navarrete-Vázquez, Gabriel
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- Regioselective synthesis of pyrimido[1,2-a][1,3,5]triazin-6-ones via reaction of 1-(6-oxo-1,6-dihydropyrimidin-2-yl)guanidines with triethylorthoacetate: Observation of an unexpected rearrangement
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A novel thermal rearrangement, involving pyrimidine ring opening and subsequent ring closure leading to recyclization of the system, was identified in the reaction of (6-oxo-1,6-dihydropyrimidin-2-yl)guanidines 3 (where NR 1R2 = NH2, NH alkyl, NH aralkyl, NHCH 2Ph(R)) with triethyl orthoacetate, affording 4-substituted-2-methyl- 6H-pyrimido[1,2-a][1,3,5]triazin-6-ones 6 and their ring opened products. However, no such rearrangement was observed with (6-oxo-1,6-dihydropyrimidin-2- yl)guanidines 3 bearing a tertiary amino or anilino substituent (i.e. where NR1R2 = N(CH3)2, indoline, morpholino, NHAr). As expected, 2-substituted-4-methyl-6H-pyrimido[1,2-a][1,3,5] triazin-6-ones 4 were obtained as the final products. Experimental structural determination and theoretical studies were carried out to get an understanding of the observed thermal rearrangement. In addition, an attempt to obtain similar pyrimido[1,2-a][1,3,5]triazin-6-ones using N,N-dimethylacetamide dimethyl acetal (DMA-DMA) as one carbon inserting synthon had furnished triazine ring annulated product 14 bearing N,N-dimethyl enamino substituent at position 4 as a result of further reaction with a second molecule of DMA-DMA.
- Sachdeva, Nikhil,Dolzhenko, Anton V.,Keung Chui, Wai
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scheme or table
p. 4586 - 4596
(2012/07/28)
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- High yielding microwave-assisted synthesis of tri-substituted 1,3,5-triazines using Pd-catalyzed aryl and heteroarylamination
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A rapid and efficient Pd-catalyzed aryl and heteroarylamination under microwave irradiation has been developed for various tri-substituted triazines that can serve as versatile building blocks for both supramolecular and medicinal chemistry research. Particularly valuable features of this method included the short reaction time, good yield, and convenient operation.
- Dao, Pascal,Garbay, Christiane,Chen, Huixiong
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scheme or table
p. 3856 - 3860
(2012/06/30)
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- 3-deoxyglucosone and skin
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The invention relates to a method of removing 3-deoxyglucosone and other alpha-dicarbonyl sugars from skin. The invention further relates to methods of inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin. The invention also relates to methods of treating 3-deoxyglucosone and other alpha-dicarbonyl sugars associated diseases and disorders of skin.
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- Biguanides and derivatives thereof as inhibitors of advanced glycosylation of a target protein
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The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
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