Product of alaptide synthesis: determination of the absolute configuration.

Alaptide is the active substance of the veterinary dermatological ointment ALAPTID and a potential drug in human medicine. Electronic circular dichroism spectroscopy (ECD), transparent spectral region optical rotation (OR), and ab initio calculations were employed to determine the absolute configuration of alaptide. No X-ray structural data determining the absolute configuration were available.

Synthesis and analgesic activity of some condensed analogs of anpirtoline.

New condensed derivatives of anpirtoline, in which the pyridine ring is replaced with quinoline, isoquinoline, quinazoline, and phthalazine nuclei, have been synthesized. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. The analgesic activity of compounds 7d, 8b, 8c, and 8e are at least comparable to that of the clinically used drugs flupirtine and tramadol under the same conditions.

[Parameters of adsorption chromatography. 5. Adsorption parameters of potential pyrimidine-type antimycotics and their correlation with biological activity].

The RF-values of 19 fungicidal pyrimidine derivatives were determined by means of thin-layer chromatography (aluminium oxide layers) in some solvent systems and the relating parameters of adsorption chromatography were calculated. Furthermore the retention times of HPLC were determined. Both of the parameters were correlated with experimentally determined biological values.