The enhancement of brain choline levels is a possible therapeutic option in neurodegenerative diseases; however, brain choline levels are held within narrow limits by homeostatic mechanisms including the rapid clearance of excess choline from the brain. The present study tests whether N-methylni...
To improve the monitoring of patients on low doses of cyclosporine there is a need for new tests of tubular function. N-1 methylnicotinamide (NMN) is an endogenous organic cation that is secreted by the proximal tubule and its clearance can be measured. In 27 patients with psoriasis, serial meas...
Substituted pyridines provide structural rigidity and thus permit the metal coordination geometry to guide the direction of propagation of the hydrogen-bonded links between building blocks. In this paper we present the crystal structures and spectroscopic properties of monomeric, dimeric and pol...
An approximate equation for differential pulse polarography, applicable to an electrodimerization process is tested with the reduction of N-methylnicotinamide. The variation of Ep with the reactant concentration is derived and tested. LSCV shows that the rate constant of the dimerization reactio...
OBJECTIVES:Nicotinamide methylation followed by urinary excretion of N-methylnicotinamide increases in cirrhotic patients, despite the derangement of the overall methylation processes in liver disease. The rise in N-methylnicotinamide could depend, at least in part, on a reduced transformation o...
Nicotinamide N-methyltransferase (NNMT), which converts nicotinamide (NA) to 1-methylnicotinamide (MNA), is up-regulated in the cirrhotic liver. Because MNA displays PGI2-dependent anti-inflammatory effects, the up-regulation of NNMT may play a regulatory role in liver inflammation. In the prese...
Nicotinamide N-methyltrasferase (NMMT) catalyzes the conversion of nicotinamide (NA) to 1-methylnicotinamide (MNA). Recent studies have reported that exogenous MNAexerts anti-thrombotic and anti-inflammatory activity, suggesting that endogenous NMMT-derived MNA may play a biological role in the ...
Using the Knudsen-effusion method and/or a diaphragm manometer static method, the vapour pressures of the condensed phases (crystalline and liquid) of nicotinamide, N-methylnicotinamide and N,N-dimethylnicotinamide were measured, respectively, over the following temperatures ranges (341.2 to 433...
The synthesis and spectral characterization of four new complexes [Cu2(5-Me-2-tpc)4(N-Menia)2] (1), [Cu(5-Me-2-tpc)2(N-Menia)2(H2O)2] (2), [Cu(3-Me-2-tpc)2(N-Menia)2]·H2O (3), and [Cu2(2-tpc)4(N-Menia)]n (4) (where 2-tpc is 2-thiophenecarboxylate, 3-Me-2-tpc is 3-methyl-2-thiophenecarboxylate, ...
BackgroundPyruvate improves contractility of normal, hypoxic, and post-ischemic myocardium. However, sodium overload is a major problem with its therapeutic application if sodium pyruvate is used. Development of alternative forms such as N-1-methylnicotinamide (MNA) pyruvate may help to overcome...
The development of antibacterial drugs based on novel chemotypes is essential to the future management of serious drug resistant infections. We herein report the design, synthesis and SAR of a novel series of N-ethylurea inhibitors based on a pyridine-3-carboxamide scaffold targeting the ATPase ...
Inhibitors of the MAP kinase p38 are potentially useful for the treatment for osteoporosis, arthritis, and other inflammatory diseases. A series of thienyl, furyl, and pyrrolyl ureas has been identified as potent p38 inhibitors, displaying in vitro activity in the nanomolar range.
Publisher SummaryThis chapter discusses carbamates/ureas. It uses two patents to discuss the topic. The first patent that is mentioned in this chapter is herbicidal sulfonylureas, their preparation, and use. The assignee for this specific patent is BASF Aktiengesellschaft and the utility designa...
C3-Symmetry tris-urea low molecular weight gelator (LMWG) (1), which shows chemical stimuli responsible for a sol–gel phase transition, was divided into five regions. Based on the division, 22 derivatives were synthesized. The gelation ability of these derivatives was tested in nine organic sol...
Thirteen novel trifluoromethylpyrazole acyl urea derivatives were designed and synthesized. In vivo fungicidal activities of these compounds were tested against Fusarium oxysporum, Corynespora mazei, Botrytis cinerea and Pseudomonas syringae respectively, particularly compounds exhibited signifi...
Biliverdin IXα is a naturally occurring linear tetrapyrrolic product of the enzymatic oxidative ring cleavage of heme. Evidence is mounting that biliverdin possesses antioxidant properties in mammals but its mode of action is unclear. We present the single crystal X-ray structure analysis of tw...
The structural formula of biologically important chiral pigments bilirubin and biliverdin differs only by one double bond. We showed that this results in dissimilar interactions with two models of membranes: cationic liposomes composed of 3β-[N-(N′,N′-dimethylaminoethane)-carbamoyl]cholestero...
Near-infrared fluorescent proteins (NIR FPs) engineered from bacterial phytochromes and their mutants with different location of Cys residues, which able to bind a biliverdin chromophore, or without these Cys residues were studied using intrinsic tryptophan fluorescence, NIR fluorescence and cir...
Biliverdin reductase-A (BVR-A) is a serine/threonine/tyrosine kinase involved in the regulation of insulin signaling. In vitro studies have demonstrated that BVR-A is a substrate of the insulin receptor and regulates IRS1 by avoiding its aberrant activation, and in animal model of obesity the lo...
The biliverdin reductase (BVR) isozymes BVRA and BVRB are cell surface membrane receptors with pleiotropic functions. This review compares, for the first time, the structural and functional differences between the isozymes. They reduce biliverdin, a byproduct of heme catabolism, to bilirubin, di...
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