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Recent Adv Antiinfect Drug Discov ; 19(3): 232-253, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38317466

RESUMO

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.


Assuntos
Antibacterianos , Testes de Sensibilidade Microbiana , Triterpenos , Ácido Ursólico , Triterpenos/farmacologia , Triterpenos/química , Humanos , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/síntese química , Células HeLa , Linhagem Celular Tumoral , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/síntese química , Bactérias/efeitos dos fármacos , Células MCF-7 , Relação Estrutura-Atividade , Simulação por Computador
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