Zero Hunger (SDG 2), Good Health & Well-being (SDG 3)
Promising activity of tetrahydroisoquinolines against multidrug-resistant clinical Salmonella isolates and cytotoxicity against monkey kidney cells Joelle Ngo Hanna* a,b , Rita A. Ndip c , Moses N. Ngemenya c,d , Casey R. Simons e , Flavien A. A. Toze b , Stephen M. Ghogomu c . James A. Mbah a* a Department of Chemistry, Faculty of Science, University of Buea, Cameroon b Department of Chemistry, Faculty of Science, University of Douala, Buea, Cameroon c Department of Biochemistry and Molecular Biology, Faculty of Science, University of Buea, Cameroon d Department of Medical Laboratory Sciences, Faculty of Health Sciences, University of Buea, Cameroon e Center for Advanced Materials Characterization in Oregon, University of Oregon, USA The high burden of Salmonella infections has been aggravated by the emergence and spread of multidrug-resistant strains affecting almost all antibiotic classes recommended for treatment. Several tetrahydroisoquinolines, both natural and synthetic, are important pharmaceuticals for a wide range of pathologies. Medicinal chemistry exploration of the tetrahydroisoquinoline scaffold has yielded analogues with considerable antimicrobial activity against bacteria, viruses, and fungi, among other pharmacological properties. We report here on a series of seventeen tetrahydroisoquinoline analogues of Dioncophyllines that were synthesized and screened against multidrug-resistant strains of Salmonella using standard methods. The cytotoxicity of selected compounds was assessed. Two compounds, 3b and 3n, were found to have activity, presenting zones of inhibition ≥ 20 mm and the best minimum inhibitory concentration (MIC) of 16 µg/mL), comparable to current anti-Salmonella drugs. Furthermore, most MBC:MIC ratios were < 4 which may indicate bactericidal activity. However, toxicity against monkey kidney cells was shown to be highly dependent on the substituent group. Further medicinal chemistry exploration based on active structures may yield a highly active antibacterial lead. Keywords: Salmonella, multidrug-resistance, tetrahydroisoquinolines, antibacterial
P31
© The Author(s), 2023
Made with FlippingBook Learn more on our blog