1341199-23-2Relevant academic research and scientific papers
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)
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.
Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors
Ma, Xiao-Dong,He, Qiu-Qin,Zhang, Xuan,Yang, Shi-Qiong,Yang, Liu-Meng,Gu, Shuang-Xi,Zheng, Yong-Tang,Chen, Fen-Er,Dai, Hui-Fang
, p. 504 - 512 (2013/02/22)
A series of N-phenylarylformamide derivatives (PAFAs) with anti-wild-type HIV-1 activity (EC50 values) ranging from 0.3 nM to 5.1 nM and therapeutic index (TI) ranging from 10 616 to 271 000 were identified as novel non-nucleoside reverse trans
