The DNA alkylating prodrug cyclophosphamide (CPA), alone or in combination with other agents, is one of the most commonly used anti-cancer agents. As a prodrug, CPA is activated by cytochrome P450 2B6 (CYP2B6), which is transcriptionally regulated by the human constitutive androstane receptor (h...
The inhibition effect of the synthesized organic compound 2-phenylimidazo [1,2-a] pyrimidine-3-carbaldehyde (IPM) on the corrosion of carbon steel (C-steel) in hydrochloric acid solution. The experiments were carried out using gravimetric (weight loss) measurements, potentio dynamic polarization...
A novel family of photochromic diarylethenes – 2,3-diarylcyclopent-2-en-1-ones (DCPs) – having high abilities to the modification reactions of ethene “bridge” is proposed. A wide series of photochromic 2,3-diarylcyclopent-2-en-1-ones have been synthesized and switch properties of obtained co...
A single crystal of (S)-(-)-2,6-diammonium-4,5,6,7-tetrahydrobenzothiazole sulfate monohydrate has been synthesized and grown at room temperature by slow evaporation of aqueous solution. The studied compound crystallizes in the space group P212121 of the orthorhombic system with cell parameters ...
Recently we have reported the effect of (S)-6-aryl urea/thiourea substituted-2-amino-4,5,6,7-tetrahydrobenzo[d]thiazole derivatives as potent anti-leukemic agents. To elucidate further the Structure Activity Relationship (SAR) studies on the anti-leukemic activity of (S)-2,6-diamino-4,5,6,7-tetr...
The design, synthesis and biological activity of a series of novel non-covalent D-Phe-Pro-Arg motif-based thrombin inhibitors incorporating 4,5,6,7-tetrahydrobenzothiazol-2-amine as a novel arginine surrogate are described. Compound 9, the most potent in the series of thrombin inhibitors, exhibi...
Nature contains things abundant in aromatic moieties which are sustained and controlled by non-covalent/aromatic interactions. Their extent of involvement provides stability and flexibility simultaneously to the systems like biological or chemical systems. Therefore, the need for designing of fl...
A method for speciation, preconcentration and separation of Fe(II) and Fe(III) in different matrices was developed using solvent extraction and flame atomic absorption spectrometry. 4-Acetyl-5-methyl-1-phenyl-1H-pyrazole-3-carboxylic acid (AMPC) was used as a new complexing reagent for Fe(III). ...
ABSTRACTAlthough choline requirements for cows are unknown, enhanced postruminal supply may decrease liver triacylglycerol and increase flux through the Met cycle to improve immunometabolic status during a negative nutrient balance (NNB). Our objectives were to investigate the effects of postrum...
Perhydro-1,4-thiazepine-4,5-dicarboxylic acid sulfoxide (cyclic cystathionine sulfoxide [cyclic cystaSO]) and N-acetylperhydro-1,4-thiazepine-3,5-dicarboxylic acid (NAc-cyclic cysta) have been identified in the urine of a patient with cystathioninuria as new metabolites of cystathionine for the ...
Hydrogen sulfide (H2S) is an endogenous neuromodulator produced mainly by the enzyme cystathionine gamma-lyase (CSE) in peripheral tissues. A pronociceptive role of endogenously produced H2S has been previously reported by our group in a model of orofacial inflammatory pain. Using the establishe...
BackgroundRegulatory cystathionine β-synthase (CBS) domains are ubiquitous in proteins, yet their mechanism of regulation remains largely obscure. Inorganic pyrophosphatase which contains regulatory CBS domains as internal inhibitors (CBS-PPase) is activated by ATP and inhibited by AMP and ADP;...
Chronic exposure of the retina to light and high concentrations of polyunsaturated fatty acid in photoreceptor cells make this tissue susceptible to oxidative damage. As retinal degenerative diseases are associated with photoreceptor degeneration, the antioxidant activity of both hydrogen sulfid...
A new method for the synthesis of cystathionine containing cyclic peptides has been developed. Conventionally such systems are typically made with relatively late-stage on-resin cyclisation involving reaction between a chlorohomoalanine and cysteine residue. We offer a different approach involvi...
A micellar liquid chromatographic method has been developed for the simultaneous determination of citalopram hydrobromide (CTA) with its two demethylated metabolites namely; desmethyl citalopram hydrochloride (DCTA) and didesmethyl citalopram tartrate (DDCTA). Separation was conducted on a C18 c...
In a previous study, we described a series of 28 aryl- and alkyl-substituted isothiouronium salts with antitumor activity and selectivity toward a leukemia cell line. Among the synthesized compounds, methyl (Z)-2-(isothioureidomethyl)-2-pentenoate hydrobromide (IS-MF08) showed conspicuous activi...
ABSTRACT:Crystal phase transition and isothermal crystallization kinetics of bupropion hydrobromide is studied by thermal analysis, X-ray powder diffractometry, and scanning electron microscopy. As well known, bupropion hydrobromide has two stable polymorphic forms, form I and form II, during th...
The crystal structure of 1-decylammonium hydrobromide was determined by X-ray crystallography. Lattice potential energy and molar volumes of the solid compound and its cation were obtained respectively. The ionic radius of the cation can be calculated from the corresponding effective volume of t...
We report on highly-sensitive ion-selective electrodes (ISEs) for potentiometric determining of galantamine hydrobromide (GB) in physiological fluids. Galantamine hydrobromide (GB) was selected for this study due to its previous medical importance for treating Alzheimer's disease. Three dif...
The solubility of Vortioxetine hydrobromide (VORH) in three binary solvent mixtures of butanone + ethanol, butanone + n-propanol, and butanone + n-butanol was determined by the gravimetric method at temperatures ranging from (283.15 to 318.15) K. Surprisingly, the solubility displays a maximum a...
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