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EN
New hydrazones of 2-(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-ylthio)acetohydrazide have been obtained and the percentages of anti/syn - conformers were determined. Based on the analyses of 1H NMR spectra, it was concluded that for hydrazones obtained from the 2- hydroxybenzaldehydes and 2’-hydroxycetophenones the ratio between the anti-and syn-conformers depends on the strength of intramolecular hydrogen bond (IMHB) between the nitrogen atom of the imino group and the proton of the 2-hydroxy group. It was shown that increase in IMHB strength results in stabilization of the anti-conformer in solution. [...]
EN
Eight hydrochlorides of 3-{2-[(2/4-fluorophenoxy)-ethylamino]}-2-hydroxypropyl-4-alkoxybenzoates and four hydrochlorides of 3-tert-butylamino-2-hydroxypropyl-4-butoxybenzoates were prepared as potential antagonists of the β1-adrenergic receptor (beta-blockers). A multistep synthesis of these compounds is described as well as their detailed analytical characterization. The pharmacokinetic properties of these weak base compounds are significantly influenced by their acid-base dissociation constant, pK a. The knowledge of this value is crucial for new drug development. This paper is aimed at developing a methodology that utilizes pH-dependent 1H NMR spectroscopy for its routine analysis. The selected predicted physico-chemical parameters of the new (arylcarbonyloxy)aminopropanols (i.e., aryloxyaminopropanol derivatives) were compared with the model drugs esmolol and flestolol. [...]
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