Enantiomeric resolution of galanthamine and related drugs used in anti-Alzheimer therapy by means of capillary zone electrophoresis employing derivatized cyclodextrin selectors.

An analytical assay is presented for the determination of the enantiomeric composition of galanthamine and related synthetic and natural compounds. (-)-Galanthamine is isolated from Galanthus nivalis and is used in this optical pure form in the therapy of Alzheimer's disease. Recent efforts for a total synthesis of unichiral (-)-galanthamine is connected with the need for a fast and reliable assay for the determination of the optical purity of the end product, as well as for optimizing and controlling the final steps in total synthesis particularly the asymmetric transformation of narwedine. In this paper the enantiomeric resolution of these compounds is reported employing a capillary electrophoretic system with beta-cyclodextrin derived chiral selectors. With the proposed system a number of galanthamine and narwedine derived analogous compounds could be separated, including 1-bromo- and N-alkyl-substituted compounds.

A facile synthesis of 1,5-diphenyl-3-(substituted oxy)-1H-1,2,4-triazoles.

A series of 1,5-diphenyl-3-alkoxy (or acyloxy)-1H-1,2,4-triazoles were synthesized and assayed in the rat adjuvant induced arthritis model. Some compounds show significant anti-inflammatory activity.

Synthesis of new 1,5-diphenyl-3-1H-1,2,4-triazoles substituted with H-, alkyl, or carboxyl groups at C-3.

Amidines obtained from benzamides and DMF- or DMA-dimethylacetal were cyclized with phenylhydrazines to 3H- or 3-methyltriazoles. 3-Ethyltriazoles were synthesized from diacylamides. Triazole-3-carboxylic acides were prepared starting from anilines. The compounds were assayed in the rat adjuvant induced arthritis model. Some compounds show significant anti-inflammatory activity.