Solid-phase Synthesis and Preliminary Evaluation of 1,6,8-Trisubstituted Tetrahydro-2H-pyrazino[1,2-a]pyrimidine-4,7-diones as a NF-kB Inhibitor

摘要

The solid-phase synthesis of new series of 1,6,8-trisubstituted tetrahydro-2H-pyrazino[1,2-a]pyrimidine-4,7-diones as bicyclic beta-turn mimetics is described.Their NF-kB inhibition activities were tested and the effect of substituents on bicyclic ring was investigated.Among the prepared compounds,the fluorobenzyl and methoxybenzyl group substituted compounds 26 and 27 at C-1 and C-8 position showed more inhibitory activities than the others.Tested at a concentration of 10 uM,these two compounds showed a 60% inhibition against the target NF kB 549.