Biomedical subjects
Publications and source records attributed to E Felder.
The optical resolution of the ammonium salt of N-acetyl-(R)(S)-p-metoxyphenylglycine was performed by differential crystallization producing the two enantiomeric forms with excellent optical purity. Hydrolysis with hydrochloric acid/hydrobromic acid yields the two enantiomers of p-methoxyphenylglycine and p-hydroxyphenylglycine respectively.
L-5-alpha-hydroxypropionylamino-2,4,6-triiodoisophthalic acid di-(1,3-dihydroxy-2-propylamide), abbreviated Iopamidol, a new non-ionic water soluble contrast agent for angiography, myelography, ventriculography and for contrast reinforced computer-assisted axial tomography is described. Extensive preclinical testing showed favorable physico-chemical features of the new compound, low systemic toxicity, excellent cardiovascular and renal tolerability, very mild effects on the blood-brain barrier and on nervous tissue.
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A series of new oral cholecystographic contrast media with promising characteristics is obtained after the study of the relationships among molecular structure, tolerability, biliary and urinary excretion, as well as gallbladder opacification. The synthesis of this series is described. Particularly good tolerability, high biliary excretion and excellent roentgenographic findings were achieved with compound (IX) (iopronic acid). This contrast agent was selected for a more detailed study of toxicology, pharmaco-kinetics, metabolism and experimental radiology.
Some physical properties of iopronic acid a new oral cholecystographic agent are reported. Determined are U.V., I.R., N.M.R. and mass spectra, X-Ray powder diffraction melting point and DTA, solubility, acidity constant and partition coefficient.
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The determination of free aromatic amine in water-soluble radiopaques by diazotization in 2-methoxyethanol-water, coupling with naphthylethylenediamine, and colorimetry of the azo dye has been automated. Sensitivity, precision, and accuracy are satisfactory for purity testing and stability studies.
A series of new heterocyclic derivatives of triiodophenyl and triiodophenoxy alkanoic acids was prepared; some of these compounds showed high billiary excretion and low acute toxicity in rats. One compound, 2-ethyl-3-[3-N-butyrolactamyl-2,4,6-triiodophenyl]-propionic acid, showed such characteristics that encouraged us to carry out further preclinical and clinical investigations.
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