1341199-24-3Relevant articles and documents
Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors
Sun, Yong,Lu, Cui-Lin,Wang, Chang-Yuan,Wang, Rui-Rui,Liu, Ke-Xin,Yang, Liu-Meng,Zhen, Yu-Hong,Zhang, Hou-Li,Wang, Chao,Zheng, Yong-Tang,Ma, Xiao-Dong
, p. 243 - 247 (2015/03/30)
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 EC50 values ranging of 0.105-14.531 μmol/L. In particular, compound 13f not only has high anti-HIV-1 activity (0.108 μmol/L), but also possesses low toxicity with a TI value of 1816.6. Furthermore, the major interactions of the inhibitor 13f 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.