ABSTRACT
We report here a simple entry into N-substituted decahydroisoxazoloquinoline system with substituents at position 3 and 4 from the readily available substrates for the first time. The synthesized isoxazoloquinolines were evaluated against six bacterial and four fungal strains. The results suggest that the decahydroisoxazolo[4,3-c]quinoline scaffold has the potential to be developed into therapeutically useful antimicrobial agents.
Subject(s)
Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Isoxazoles/chemistry , Nitrogen/chemistry , Quinolines/chemistry , Quinolines/pharmacology , Bacteria/drug effects , Fungi/drug effectsABSTRACT
The present Letter describes a one-pot multi-component method that allows the efficient and mild preparation of 3,5-diphenylpiperidin-2,6-dione and a new series of 3,5-diarylpiperidin-2,6-dione derivatives from ethyl 2-arylacetates, formaldehyde and ammonia/aliphatic/aromatic amines. The structures of the compounds were elucidated by IR, NMR spectroscopic data and microanalyses. The anticonvulsant activities of these compounds were evaluated by maximal electroshock seizure test and were also evaluated for motor impairment. Among the synthesized compounds, 5a, 5b, 5d, and 5e could be considered potentially the most useful and safe therapeutic compound and 5g, 5i, 5j, 5m, and 5o exhibit potent activities.
