A series of octahydroquinazoline-5-ones as novel inhibitors against dengue virus.

摘要: Abstract A series of octahydroquinazoline-5-ones (OHQs 1–50) were designed and synthesized via an improved five-component reaction (5CR). Their bioactivities against dengue virus (DENV) evaluated by determining lacate dehydrogenase (LDH) in the BHK-21 cells infected with DENV-2. Primary structure-activity relationship showed that six OHQs suitable substituents displayed good activities EC50 = 1.31–1.85 μM. The primary bioactivity mechanism was investigated using most potent OHQ 23. Experimental results indicate 23 could efficiently reverse DENV-2-induced cytopathic effect suppress expression viral structure E protein, but no interaction MTase RdRp domain NS5, a protein plays important role genome transcription translation. efficient synthetic method, novel structures as DENV inhibitors are expected to be developed potential inhibitors.