Novel 16-substituted bifunctional derivatives of huperzine B: multifunctional cholinesterase inhibitors

Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors.

In the process of optimization, we developed a novel core skeleton of thieno[3,4-b]pyrazine via GK-13. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-b]pyrazine derivatives were shown to exhibit promising activity for use as potential therapeutic small-molecules in renal cancer by inh...

Design, synthesis and evaluation of difunctionalized 4-hydroxybenzaldehyde derivatives as novel cholinesterase inhibitors.

A series of difunctionalized 4-hydroxybenzaldehyde derivatives were designed, synthesized and evaluated as cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)) inhibitors. The results demonstrated that all the compounds had more potent AChE and BChE inhibitory activities than galanthamine-HBr, one of the best cholinesterase inhibitors known so far. The inhibition mechan...

Synthesis and biological evaluation of substituted phenylpyrazole[4,5-b]oleanane derivatives as inhibitors of glycogen phosphorylase.

A series of substituted phenylpyrazole[4,5-b]oleanane derivatives have been synthesized and biologically evaluated as inhibitors of glycogen phosphorylase (GP). The structure of phenylpyrazole moiety in compound 17 was determined by ROESY. All of the synthesized oleanane derivatives were biologically evaluated against rabbit muscle GPa. Within this series of compounds, pyrazole triterpene 7 (IC...

Multifunctional Characteristics of B-site Substituted BiFeO3 Films

Novel substituted heteroaromatic piperazine and piperidine derivatives as inhibitors of human enterovirus 71 and coxsackievirus a16.

A series of substituted heteroaromatic piperazine and piperidine derivatives were found through virtual screening based on the structure of human enterovirus 71 capsid protein VP1. The preliminary biological evaluation revealed that compounds 8e and 9e have potent activity against EV71 and Coxsackievirus A16 with low cytotoxicity.