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Biomedical subjects

E Schrötter

Publications and source records attributed to E Schrötter.

16 recordsLinked to original sources
PubMed1986

[The synthesis of 3-amino-5-(4-pyridinyl)-1,2-dihydropyrid-2-one (Cordemcura) from a technical mixture of pyridines].

For preclinical and clinical research the headline compound 6 has been synthesized from pyrid-4-yl-malondialdehyde (3) and its bis-N,N-dimethyl)-aldimin-derivative 1 by cyclization with cyanoacetamide giving 4, partial hydrolysis to the amide 5, and degradation by sodiumhypochlorite to the amine 6, concerning to the way described in patent literature. Starting product was a mixture of alkyl pyridines from which 4-picoline reacted selectively with the Vilsmeyer-complex of phosgene/DMF to give cristalline 1. Optimization in all steps resulted in a procedure that gives us the intermediates in good yields and qualities and the final product 6 with high purity, suitable for pharmaceutical use.

Aminopyridines↗
PubMed1983

[Substituted picolinic acids as DBH inhibitors. Inhibition of dopamine beta-hydroxylase and antihypertensive action].

The authors determined the dissociation constant, the constant of copper complex formation, the inhibitory action on the catecholamine biosynthesis enzyme dopamine beta-hydroxylase (DBH; copper glycoprotein), as well as the antihypertensive effect on spontaneously hypertensive rats of a series of substituted picolinic or fusaric acids (FA; 5-n-butylpicolinic acids). The substances investigated may be characterized as weak to medium-strong acids which form stable copper(II) complexes in solution and in the solid state. The concentrations required for a 50% inhibition of DBH range between 10(-6) and 10(-5) mol/l. The picolinic acid structure is of greater importance to enzyme inhibition than the butylpyridine structure. From the inhibition type of FA it may be deduced that the mechanism of inhibition cannot be explained only by the complex formation of the enzyme copper. Most of these derivatives are of hypotensive activity; some others exert a hypertensive effect. A quantitative correlation between the action on blood pressure and the enzyme inhibition cannot be established without calculation (quantitative structure-activity analysis). The hypotensive activity is above all due to DBH inhibition in the angiovascular region and in the suprarenal gland.

Animals↗