IntroductionCreatine is an amino acid derivative that is involved in preserving ATP homeostasis. Previous studies suggest an important role for the creatine kinase circuit for placental ATP turnover. Creatine is obtained from both the diet and endogenous synthesis, usually along the renal-hepati...
Traumatic brain injury (TBI) is a devastating disease frequently followed by behavioral disabilities including post-traumatic epilepsy (PTE). Although reasonable progress in understanding its pathophysiology has been made, treatment of PTE is still limited. Several studies have shown the neuropr...
BackgroundCerebral Creatine deficiency syndromes (CCDS) include three hereditary diseases affecting the metabolism of creatine (Cr): arginine glycine amidinotransferase deficiency, guanidinoacetate methyltransferase deficiency and disorders of creatine transporter. These pathologies cause a brai...
Synthesis of 7-amino-1,3-dioxo-1,2,3,5-tetrahydropyrazolo[1,2-a][1,2,4]triazole derivatives by a three component reaction of aryl aldehydes, 4-phenylurazole and malononitrile or ethyl cyanoacetate in the presence of catalytic amount of weak basic ionic liquids such as N-butyl-N-methylpyrrolidini...
Phosphodiesterase 10A (PDE10A) inhibitors were designed and synthesized based on the dihydro-imidazobenzimidazole scaffold. Compound 5a showed moderate inhibitory activity and good permeability, but unfavorable high P-glycoprotein (P-gp) liability for brain penetration. We performed an optimizat...
Isoxazolines 2 from the cycloaddition of imidazoline 3-oxides 1 with DMAD rearrange in the presence of methoxide to give cis-3-methoxy-7-(methoxycarbonyl)-2,7a-diaryl-5-oxo-2,3,5,7a-tetrahydro-1H-pyrrolo[1,2-e]imidazol-6-olates 3 with 100% de. The acidic hydrolysis of 3 led to kinetically contro...
The reactions of (aryl)(chloro)methyl p-tolyl sulfoxides 2 with tetrasulfur tetranitride (S4N4) in p-dioxane at reflux gave 3,5-diaryl-1,2,4,6-thiatriazine 1-oxides, 3,5-diaryl-1,2,4-thiadiazoles, and 1-amino-3,5-diaryl-1,2,4,6-thiatriazine 1-oxides. For the first time, the structures of 3,5-dia...
Three benzoxazines (7–9) with a tolyl, p-hydroxyphenyl or p-carboxyphenyl structure, respectively, were successfully synthesized by a three-pot or two-pot procedure. In the three-pot approach, the first step is the condensation of 2-hydroxybenzaldehyde with p-toluidine, 4-aminophenol and 4-amin...
Perfluoro-n-octylmagnesium bromide has been conveniently synthesized through the metal-halogen exchange reaction between perfluoro-n-octyl iodide and ethyl- or phenyl-magnesium bromide. The thermal stability of the Grignard reagent and the products of the thermal decomposition have been estimate...
Transglycosylase (TGase) is essential to biosynthesis of peptidoglycan for formation of bacterial cell wall. Moenomycin is a potent TGase inhibitor, but not used in clinic treatment due to its poor pharmacokinetics. The E−F disaccharide, phosphoglycerate and lipid tail in moenomycin are crucial ...
A convenient large-scale chiral synthesis of protected 2-substituted-4-oxo-piperidine derivatives is described. Hetero Diels–Alder reaction between trifluoroacetic acid–boron trifluoride activated (1-phenyl-ethylimino)acetic acid ethyl ester and 2-trimethylsilyloxy-1,3-butadiene gave rise to a...
Control of the chemical structure of copolyimides through the sequence control of copolyamic acid methyl esters was tried. The copolyamic acid methyl esters were directly synthesized from 2,5-dicarbomethoxy terephthalic acid (p-PMDE) and two diamines, 4,4′-oxydianiline (ODA) and 2,2′-bis (trif...
Both stereoisomers of β-(2-phenylethoxy)vinyl-λ3-iodane and (Z)-β-aroyloxyvinyl-λ3-iodane were prepared stereoselectively. These substituted vinyl-λ3-iodanes undergo nucleophilic vinylic substitutions with n-Bu4NX (X=Cl, Br, I) under mild conditions, yielding vinyl halides. The observed inv...
The first-order UV-derivative spectrophotometry, applying zero-crossing method was developed for the determination of omeprazole (OM), omeprazole sulphone (OMS), pantoprazole sodium salt (PANa), and N-methylpantoprazole (NPA) in methanol–ammonia 4.0% v/v, where the sufficient spectra resolution...
The therapeutic potential of saquinavir, a specific inhibitor of human immunodeficiency virus (HIV)-1 and HIV-2 protease enzymes, has been largely limited because of a low solubility and consequnt low bioavailability. Thus, we aimed to design a supersaturated self-microemulsifying drug delivery ...
The performance of lithium ion batteries (LIBs) is highly dependent on the properties of the anode materials. Developing new carbon materials and metal oxides/sulfides with high capacities has attracted growing attention due to the limited theoretical capacity of commercial graphite. Pyrite (FeS...
Lithium-sulfur battery has emerged as one of the greatest battery technologies because of its high energy density, however, the cycling performance is not satisfied mainly due to the dissolution of lithium polysulfides. To solve this problem, herein CoSx in a composite with nitrogen doped carbon...
A novel nanohybrid based on palladium sulfide nanoparticles uniformly dispersing on heterostructure of MoS2/nitrogen-doped graphene (PdxSy-MoS2/N-GR) was developed for catalyzing oxygen reduction reaction in alkaline medium. The nanohybrid demonstrated effectively catalytic performance with a po...
Designing a hybrid architecture of electroactive species on the modified graphene sheets is one of the most promising tactics for high-performance supercapacitors. Herein, multiphase nickel sulfides nanoparticles (Ni3S2-NiS, abbreviated as Ni-S-1) with abundant edge sites were synthesized by pyr...
Rod-like porous composites of iron sulfides embedded in nitrogen-rich carbon have been synthesized through a simultaneous carbonization and sulfuration process of the Fe-based metal-organic framework (MIL-88) for the first time. The composites exhibit combined advantages of the porous structure,...
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