Determination of the Dissociation Constant of a Weak Acid Using a Dissolution Rate Method

Hansen, Jørgen B.; Häfliger, O.

doi:10.1002/jps.2600720426

Cited by 16 publications

(8 citation statements)

References 12 publications

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“…The commonly used methods for the determination of dissociation constants include potentiometric titration [5], UV-Vis spectrophotometric titration [6], conductivity [7], thermodynamics [8], nuclear magnetic resonance spectroscopy [9], dissolution rate method [10], ionophoretic techniques [11], and isotachophoresis (ITP) [12,13]. All the abovementioned methods have some limitations, such as the carbonate-free buffer, the concentration and solubility of the analyte, the conductivity and pH value of the electrolyte.…”

Section: General Considerationsmentioning

confidence: 99%

Determination of pKa values of anthraquinone compounds by capillary electrophoresis

2001

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In this paper, the dissociation constants (pKa1, pKa2) of five anthraquinones were determined from the relation between the effective mobility at different pH values and the buffer pH value, which was derived from the basic electrophoresis theory and the dissociation equilibrium of a binary acid. In addition, the changes of pKa values of the five compounds were also investigated when organic modifiers were added to the buffer system.

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Section: General Considerationsmentioning

confidence: 99%

Determination of pKa values of anthraquinone compounds by capillary electrophoresis

2001

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“…Ro 13-3978 has high metabolic stability, 3,4 but when we administered a 100 mg/kg oral dose of this aryl hydantoin to mice, we observed low levels of hydroxymethyl metabolite 1 and urea carboxylic acid 2 , the hydantoin hydrolysis product 5 (Figure 1). Based on AUC 0-24h values, the respective exposures of 1 and 2 were 3 and <1% relative to that of Ro 13-3978.…”

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confidence: 93%

SAR of a new antischistosomal urea carboxylic acid

Wang

Häberli

et al. 2018

Bioorganic & Medicinal Chemistry Letters

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Urea carboxylic acids, products of aryl hydantoin hydrolysis, were recently identified as a new antischistosomal chemotype. We now describe a baseline structure-activity relationship (SAR) for this compound series. With one exception, analogs of lead urea carboxylic acid 2 were quite polar with LogD7.4 values ranging from −1.9 to 1.8, had high aqueous solubilities in the range of 25-100 μg/mL, and were metabolically stable. None of the compounds had measurable in vitro antischistosomal activity or cytotoxicity, but four of these had moderate worm burden reduction (WBR) values of 42-70% when they were administered as single 100 mg/kg oral doses to S. mansoni-infected mice. These data indicate that with the exception of the gem-dimethyl substructure and the distal nitrogen atom of the urea functional group, the rest of the structure of 2 is required for in vivo antischistosomal activity.

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“…The methods for the determination of the dissociation constant include potentiometric titration [1±4], UV-Vis spectrophotometric titration [5±8], conductivity [9], thermodynamics [10±11], nuclear magnetic resonance spectroscopy [12,13], dissolution rate method [14], ionophoretic techniques [15,16], isotachophoresis (ITP) [17,18] and capillary electrophoresis (CE) [19±24]. The widely used methods for the determination of the dissociation constant in aqueous phase are potentiometric titration and UV-Vis spectrophotometric titration.…”

Section: Introductionmentioning

confidence: 99%

Determination of dissociation constants of amino acids by capillary zone electrophoresis

Yang

Yuan

1999

Electrophoresis

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Determination of the Dissociation Constant of a Weak Acid Using a Dissolution Rate Method

Cited by 16 publications

References 12 publications

Determination of pKa values of anthraquinone compounds by capillary electrophoresis

Determination of pKa values of anthraquinone compounds by capillary electrophoresis

SAR of a new antischistosomal urea carboxylic acid

Determination of dissociation constants of amino acids by capillary zone electrophoresis

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