1,5-Disubstituted indazol-3-ols with anti-inflammatory activity.

A series of new indazol-3-ol derivatives was synthesized. Some of these compounds exhibit interesting anti-inflammatory activities in various models of inflammation. 5-Methoxy-1-[quinoline-2-yl-methoxy)-benzyl]-1H-indazol-3-ol (27) strongly inhibits the oxidation of arachidonic acid to 5-hydroperoxyeicosatetraenoic acid catalyzed by 5-lipoxygenase (IC50 = 44 nM).

Enantioselective high-performance liquid chromatography assay of (+)R- and (-)S-alpha-lipoic acid in human plasma.

A specific plasma level assay for the enantiomers of alpha-lipoic acid is described. It makes use of liquid-liquid extraction, chemical reduction to the dithiol enantiomers, and their precolumn chiral derivatisation with o-phthalaldehyde in the presence of D-phenylalanine. The two diastereomeric derivatives are separated by reversed-phase HPLC with fluorescence detection.

Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds.

In the course of studies on tranquilizers, new non-benzodiazepine-like compounds were synthesized. These are 1-(3,4,5-trimethoxyphenoxy)-3-[4-(2-methoxyphenyl)piperazinyl]prop an-2-ol (INN: enciprazine) and derivatives thereof which were screened pharmacologically in order to evaluate their central nervous system activity. Compounds with marked antiaggressive and anxiolytic properties but without dependence potential could be detected.

Studies on the Origin of (-)-alpha-Bisabolol and Chamazulene in Chamomile Preparations; Part I. Investigations by Isotope Ratio Mass Spectrometry (IRMS).

IRMS was used to determine the delta (13)C-and deltaD-values of dried plant material and essential oil fractions of CHAMOMILLA RECUTITA and VANILLOSMOPSIS ERYTHROPAPPA and of isolated components thereof. Both plants turned out to follow the same C (3) photosynthetic pathway. The carbon isotope ratios ( delta (13)C-values) of chamomile-derived bisabolol ranged from -32 per thousando to -30 per thousand; the corresponding deltaD-values varied between -240 per thousand and -205 per thousand.