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

ABSTRACT: 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 IC₅₀ values of 4b and 5f were 0.49 ± 0.11 μM and 0.39 ± 0.13 μM in

SUBMITTER: Khuzwayo SS 

PROVIDER: S-EPMC11883425 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature