In the present study,novel ester derivatives of CAPE were designed and synthesized as neuroprotective agents.The anti-inflammatory and antioxidant activities of these compounds were evaluated at the cellular level,whi...In the present study,novel ester derivatives of CAPE were designed and synthesized as neuroprotective agents.The anti-inflammatory and antioxidant activities of these compounds were evaluated at the cellular level,while the blood-brain barrier(BBB)permeability was predicted by parallel artificial membrane permeability assay(PAMPA).The results revealed that phenolic hydroxyl groups and double bonds in the structure of CAPE had important effects on neuroprotective activities.Accordingly,a preliminary structure-activity relationship was summarized in this paper.In addition,we observed a significant improvement on BBB permeability.These results provided important references for the structural modification and optimization of CAPE in the future.展开更多
Three series of novel anti-immunodeficiency virus 1 （HIV-1） dual （RT/1N） inhibitors were rationally designed by introducing a functioning diketo acid （DKA） into pyridin-2-one scaffold. To efficiently analyze inh...Three series of novel anti-immunodeficiency virus 1 （HIV-1） dual （RT/1N） inhibitors were rationally designed by introducing a functioning diketo acid （DKA） into pyridin-2-one scaffold. To efficiently analyze inhibitory activity, these compounds were screened against HIV-1 RT and IN respectively via surface plasmon resonance （SPR）, and active compounds were subsequently evaluated by enzyme assay. It was noteworthy that compound A2 exhibited moderate activity against both HIV-1 RT and IN. This result provided information for further development of pyridinone analogues as potent dual HIV-1 inhibitors.展开更多
文摘In the present study,novel ester derivatives of CAPE were designed and synthesized as neuroprotective agents.The anti-inflammatory and antioxidant activities of these compounds were evaluated at the cellular level,while the blood-brain barrier(BBB)permeability was predicted by parallel artificial membrane permeability assay(PAMPA).The results revealed that phenolic hydroxyl groups and double bonds in the structure of CAPE had important effects on neuroprotective activities.Accordingly,a preliminary structure-activity relationship was summarized in this paper.In addition,we observed a significant improvement on BBB permeability.These results provided important references for the structural modification and optimization of CAPE in the future.
基金National Natural Science Foundation of China(Grant No.21172014,812111023 and 81172733)grants from the Ministry of Science and Technology of China(Grant No.200 9ZX09301-010)
文摘Three series of novel anti-immunodeficiency virus 1 （HIV-1） dual （RT/1N） inhibitors were rationally designed by introducing a functioning diketo acid （DKA） into pyridin-2-one scaffold. To efficiently analyze inhibitory activity, these compounds were screened against HIV-1 RT and IN respectively via surface plasmon resonance （SPR）, and active compounds were subsequently evaluated by enzyme assay. It was noteworthy that compound A2 exhibited moderate activity against both HIV-1 RT and IN. This result provided information for further development of pyridinone analogues as potent dual HIV-1 inhibitors.
