摘要：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.