Citation: Yong Sun, Cui-Lin Lu, Chang-Yuan Wang, Rui-Rui Wang, Ke-Xin Liu, Liu-Meng Yang, Yu-Hong Zhen, Hou-Li Zhang, Chao Wang, Yong-Tang Zheng, Xiao-Dong Ma. Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors[J]. Chinese Chemical Letters, ;2015, 26(2): 243-247. doi: 10.1016/j.cclet.2014.11.004 shu

Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors

1.
a College of Pharmacy, Dalian Medical University, Dalian 116044, China;
2.
b Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China;
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c Kunming College of Life Science, University of Chinese Academy of Sciences, Kunming 650204, China

Corresponding author: Yong-Tang Zheng, Xiao-Dong Ma,
Received Date: 2 September 2014
Available Online: 23 October 2014
Fund Project: This work was supported in part by grants from the National Natural Science Foundation of China (No. 81402788) (No. 81402788)

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 mmol/L. In particular, compound 13f not only has high anti-HIV-1 activity (0.108 mmol/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.
- Benzophenone,
- N-Phenylbenzenesulfonamide,
- Structure modification,
- Anti-HIV activity
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