Non-nucleoside reverse transcriptase inhibitors (NNRTIs) exhibit promising anti-HIV-1 activities, however, their effectiveness is limited by drug resistant mutations, low solubility, and drug-drug interactions. Here, the authors develop a series of piperazine sulfonyl-bearing diarylpyrimidine based NNRTIs which show improved potency against HIV-1 by enhancing backbone-binding interactions.
- Xiangyi Jiang
- Boshi Huang
- Peng Zhan