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Recent Advances in Anti-Infective Drug Discovery

Editor-in-Chief

ISSN (Print): 2772-4344
ISSN (Online): 2772-4352

Research Article

Synthesis of Ursolic Acid-based Hybrids: In Vitro Antibacterial, Cytotoxicity Studies, In Silico Physicochemical and Pharmacokinetic Properties

Author(s): Vuyolwethu Khwaza, Samson Olaitan Oselusi, Eric Morifi, Mutshinyalo Nwamadi, Kamogelo S. Hlope, Derek Tantoh Ndinteh, Thabe Moses Matsebatlela, Opeoluwa Oyehan Oyedeji and Blessing Atim Aderibigbe*

Volume 19, Issue 3, 2024

Published on: 02 January, 2024

Page: [232 - 253] Pages: 22

DOI: 10.2174/0127724344272444231114103144

Price: $65

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Abstract

Background: There is a critical need for the discovery of novel and effective antibacterial or anticancer molecules.

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.

Graphical Abstract

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