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Design and synthesis of oxaprozin‐1,3,4‐oxadiazole hybrids as potential anticancer and antibacterial agents
20
Citations
36
References
2020
Year
Antibacterial AgentsAntibacterial ActivityOrganic ChemistryPharmacotherapyChemistryHeterocycle ChemistryPharmaceutical ChemistryPotential AnticancerDrug ResistanceMedicinal ChemistryDiversity Oriented SynthesisAnti-cancer AgentDerivativesSeries 5CDrug DevelopmentPharmacologyOxaprozin‐1,3,4‐oxadiazole HybridsGood Antibacterial ActivityNatural SciencesMedicineSynthetic ChemistrySmall MoleculesDrug Discovery
Abstract In the present study, we report design, synthesis and screening of new novel 5‐substituted‐2‐mercapto‐1,3,4‐oxadiazole analogues appended to oxaprozin for their in vitro anticancer and antibacterial activity. The synthesised compounds were characterized using various spectroscopic techniques. Furthermore, the structure of 5b (2‐(2‐[4,5‐diphenyloxazol‐2‐yl]ethyl)‐5‐(ethylthio)‐1,3,4‐oxadiazole) was unequivocally confirmed by X‐ray analysis. Among the series 5c (2‐(2‐[4,5‐diphenyloxazol‐2‐yl]ethyl)‐5‐(propylthio)‐1,3,4‐oxadiazole) showed most promising anticancer activity against A549 cancer cell line and all the reported analogues manifested satisfactory safety profiles against human normal cell line HEK293T. The products exhibited good antibacterial activity and among the tested 5j (2‐(2‐[4,5‐diphenyloxazol‐2‐yl]ethyl)‐5‐([4‐fluorobenzyl]thio)‐1,3,4‐oxadiazole) exhibited most potent.
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