Searching for more safe and effective agents for HIV treatments is still an urgent topic worldwide.Based on our continuous modifications on the benzophenone derivatives as HIV-1 reverse transcriptase（RT）inhibitors,a...Searching for more safe and effective agents for HIV treatments is still an urgent topic worldwide.Based on our continuous modifications on the benzophenone derivatives as HIV-1 reverse transcriptase（RT）inhibitors,a new template bearing N-phenylbenzenesulfonamide（PBSA） structure was designed to enhance the interactions with HIV-1 RT.In this manuscript,a series of PBSA derivatives were synthesized and evaluated for their anti-HIV-1 activity.The preliminary test showed that these compounds were potent to inhibit wild-type HIV-1 with EC_（50） values ranging of 0.105-14.531 μmol/L.In particular,compound 13 f not only has high anti-HIV-1 activity（0.108 μmol/L）,but also possesses low toxicity with a Tl value of 1816.6.Furthermore,the major interactions of the inhibitor 13 f with HIV-1 RT were also investigated using the molecular modelling.Our discovered structure-activity relationships（SARs） of these analogues may serve as an important clue for further optimizations.展开更多
基金supported in part by grants from the National Natural Science Foundation of China(No.81402788)the Ph.D. Start-up Fund of Natural Science Foundation of Liaoning Province, China(No.20141115)
文摘Searching for more safe and effective agents for HIV treatments is still an urgent topic worldwide.Based on our continuous modifications on the benzophenone derivatives as HIV-1 reverse transcriptase（RT）inhibitors,a new template bearing N-phenylbenzenesulfonamide（PBSA） structure was designed to enhance the interactions with HIV-1 RT.In this manuscript,a series of PBSA derivatives were synthesized and evaluated for their anti-HIV-1 activity.The preliminary test showed that these compounds were potent to inhibit wild-type HIV-1 with EC_（50） values ranging of 0.105-14.531 μmol/L.In particular,compound 13 f not only has high anti-HIV-1 activity（0.108 μmol/L）,but also possesses low toxicity with a Tl value of 1816.6.Furthermore,the major interactions of the inhibitor 13 f with HIV-1 RT were also investigated using the molecular modelling.Our discovered structure-activity relationships（SARs） of these analogues may serve as an important clue for further optimizations.
