Design and synthesis of β-carboline-benzofuran based hybrids as antibacterial agents against Staphylococcus aureus
Year: 2025
Type: article
Abstract: The significant threat posed by Staphylococcus aureus (MRSA) is attributed to various antibiotic resistance and its role in severe infections. As an approach to combat this, a series of novel β-carboline-benzofuran based molecular hybrids were designed, synthesized, and evaluated for their antibacterial activity against Staphylococcus aureus ATCC 29213. Among the series, the minimum inhibitory concentration (MIC) of key compounds 13e , 13 h , and 13q was determined to be 4 μg/mL, compared to ciprofloxacin 0.125 μg/mL. The docking results also supported the potent compounds' ability to inhibit DNA gyrase . These compounds demonstrated bacteriostatic effects at higher concentrations, with significant inhibition of biofilm formation (MBIC 50 ranging from 12.78 to 30.68 μg/mL). Additionally, the compounds displayed minimal cytotoxicity against HepG2 cells and inhibited DNA gyrase , which is proven by DNA supercoiling assays and molecular docking studies. In addition, ADMET predictions indicated favorable drug-like properties, adhering to Lipinski's rule of five . These findings suggest that the synthesized β-carboline-benzofuran hybrids possess significant potential as leads for developing new antibacterial agents against MRSA .
Authors: Mursalim Ali Khan, Kishan Kumar Parida, Dastari Sowmya, Naveen Chand Rallabandi, Nitin Pal Kalia, Nagula Shankaraiah
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: hybrid
Estimated APC paid: $3,880
OpenAlex ID: W4409200141