Development of 1,2,3-triazole-based sphingosine kinase inhibitors and their evaluation as antiproliferative agents
Two series of N-(aryl)-1-(hydroxyalkyl)pyrrolidine-2-carboxamides (2a-2g and 3a-3g) and 1,4-disubstituted 1,2,3-triazoles (5a-5h and 8a-8h) were synthesized. All the compounds, containing a lipophilic tail and a polar headgroup, were evaluated as sphingos
Synthesis and analgesic evaluation of a series of proline-typed spiro cyclic quaternary ammoniums
A series of proline derivated spirocyclic quaternary ammoniums were synthesized and evaluated via in vivo analgesic activities. Compounds 9a showed the best analgesic effect with 84 % inhibition in mice. These compounds showed only micromolar Ki value by in vitro α7 nAChR binding test, which may indicate the form of active metabolite play a role in their in vitro analgesic activities.