Recent Advances in Anti-Infective Drug DiscoveryRecent Advances in Anti-Infective Drug DiscoveryRecent Advances in Anti-Infective Drug Discovery2772-43442772-4344Bentham Science64455910.2174/0127724344272444231114103144MedicineResearch ArticleSynthesis of Ursolic Acid-based Hybrids: In Vitro Antibacterial, Cytotoxicity Studies, In Silico Physicochemical and Pharmacokinetic PropertiesKhwazaVuyolwethuinfo@benthamscience.netOselusiSamsoninfo@benthamscience.netMorifiEricinfo@benthamscience.netNwamadiMutshinyaloinfo@benthamscience.netHlopeKamogeloinfo@benthamscience.netNdintehDerekinfo@benthamscience.netMatsebatlelaThabeinfo@benthamscience.netOyedejiOpeoluwainfo@benthamscience.netAderibigbeBlessinginfo@benthamscience.netDepartment of Chemistry, University of Fort HareSchool of Pharmacy, University of the Western CapeSchool of Chemistry, Mass Spectrometry Division, University of WitwatersrandDepartment of Chemistry, University of JohannesburgDepartment of Biochemistry, Microbiology and Biotechnology, Faculty of Science and Agriculture, University of LimpopoDepartment of Applied Chemistry, University of Johannesburg0103202419323225307012025Copyright ©; 2024, Bentham Science Publishers2024Bentham Science Publishershttps://journals.eco-vector.com/2772-4344/article/view/644559

Background:Background

Objectives:Amine-linked ursolic acid-based hybrid compounds were prepared in good yields in the range of 60-68%.

Methods:Their molecular structures were successfully confirmed using different spectroscopic methods including 1H/13C NMR, UHPLC-HRMS and FTIR spectroscopy. The in vitro cytotoxicity of some of these hybrid molecules against three human tumour cells, such as MDA-MB23, MCF7, and HeLa was evaluated using the MTT colorimetric method.

Result:Their antibacterial efficacy was evaluated against eleven bacterial pathogens using a serial dilution assay. Majority of the bacterial strains were inhibited significantly by compounds 17 and 24, with the lowest MIC values in the range of 15.3-31.25 µg/mL. Compound 16 exhibited higher cytotoxicity against HeLa cells than ursolic acid, with an IC50 value of 43.64 g/mL.

Conclusion:The in vitro antibacterial activity and cytotoxicity of these hybrid compounds demonstrated that ursolic acid-based hybrid molecules are promising compounds. Further research into ursolic acid-based hybrid compounds is required.

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