2,3-Diaminopyridine reacts with cyclohexanone to form dihydro-4-azabenzimidazole-2-spirocyclohexane. Reaction of this intermediate with a variety of nucleophiles (e.g., water, phenylmercaptan, ethanol, dimethylamine, and diethylmalonate) in the presence of MnO2 results in addition to the 5-position. Subsequent acidic hydrogenation affords 6-substituted-2,3-diaminopyridines, key synthons for the synthesis of bicyclic heterocycles.
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.
A series of 5-azaquinoxaline-2,3-dione derivatives were synthesized and evaluated on d-amino acid oxidase (DAAO) inhibition as potential α-hydroxylactam-based inhibitors. The potent inhibitory activities in vitro suggested that 5-nitrogen could significantly enhance the binding affinity by strengthening relevant hydrogen bond interactions. The analgesic effects of intrathecal and systemic injection
合成了一系列5-氮杂喹喔啉-2,3-二酮衍生物,并评估了其作为潜在的基于α-羟基内酰胺的抑制剂对d-氨基酸氧化酶(DAAO)的抑制作用。体外的强抑制活性表明5-氮可以通过增强相关的氢键相互作用来显着增强结合亲和力。研究了鞘内和全身注射8-氯-1,4-二氢吡啶并[2,3- b ]吡嗪-2,3-二酮(5-氮杂喹喔啉-2,3-二酮的代表分子)的镇痛作用。啮齿动物。这项研究不仅证实了DAAO抑制剂的镇痛作用,而且还提供了一类具有口服应用潜力的新型化学实体,可用于治疗慢性疼痛和吗啡镇痛耐受性。
Fructoseamine 3 kinase and the formation of collagen and elastin
申请人:Tobia Annette
公开号:US20070065443A1
公开(公告)日:2007-03-22
The invention relates to the discovery that levels of collagen and elastin can be modulated by changing the flux through the Amadori Pathway and that copper containing compounds and complexes inhibit the enzyme fructoseamine-3-kinase.
Method for reducing a susceptibility to tumor formation induced by 3-deoxyglucosone and precursors thereof
申请人:Brown R. Truman
公开号:US20060089316A1
公开(公告)日:2006-04-27
Disclosed are methods of using various compounds, which are known to bind to 3-deoxyglucosone (3DG) or precursors thereof, in order to reduce a susceptibility to tumor formation and/or to prevent or delay onset of tumor formation induced by 3DG and its precursors. Also disclosed is the reduction of 3DG levels in high fructose corn syrop so that the high fructose corn syrup is less likely to induce tumor formation.
Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.