The synthesis and investigation of novel 3-benzoylbenzofurans and pyrazole derivatives for anti-HIV activity.

• Tác giả: Ntombenhle H Gama, Sinothile S Khuzwayo, Debra Meyer, Mamoalosi A Selepe
• Ngôn ngữ: eng
• Ký hiệu phân loại: 940.27 $Period of French Revolution and Napoleon I, 1789-1815
• Thông tin xuất bản: England : RSC medicinal chemistry , 2025
• Bộ sưu tập: NCBI
• ID: 683304

Tóm tắt

The emergence of drug-resistant viruses continues to be an obstacle to effectively controlling the HIV/AIDS pandemic. The development of novel drugs with high potency and the ability to fully eradicate HIV-1 infections is therefore of critical importance. Novel pyrazole derivatives were synthesized from 3-benzoylbenzofurans and characterized by mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopy. The 3-benzoyl benzofurans were determined to be highly cytotoxic in TZM-bl cells, while their pyrazole derivatives were mild to non-cytotoxic. Evaluation of anti-HIV activities in pseudoviruses revealed two 3-benzoyl benzofurans (3g and 4b) and pyrazoles (5f and 5h) as the most potent inhibitors. The IC