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SYNTHESIS OF NEW BENZYLIDENEHYDRAZINYLPHENYLTHIAZOLES AND EVALUATION OF THEIR ANTIINFLAMMATORY ACTIVITY IN VITRO AND METABOLIC STABILITY

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dc.contributor.authorTAN JOE JEN
dc.date.accessioned2023-10-06T15:25:29Z
dc.date.available2023-10-06T15:25:29Z
dc.date.issued2021
dc.description.abstractHydrazones and thiazoles possess a wide spectrum of biological activities including antimicrobial, anticonvulsant, analgesic, anti-inflammatory, antiplatelet, antitubercular and antitumour activities. Acyl hydrazones with an azomethine proton (-NHN=CH-) possess promising biological activities and existence ofthiazole bearing anti-inflammatory drugs such as Fanetizole, Meloxicam and Fentiazac prompted us to design new benzylidenehydrazinylphenylthiazoles (BHPT). BHPT compounds were synthesised via condensation of thiosemicarbazide with aryl aldehyde, followed by cyclisation in the presence of aryl substituted 2-bromo-l-phenylethan-1-ones. The compounds were characterised using UV-VIS, FT-IR, 1H & 13C NMR, and LC-MS techniques. Anti-inflammatory activity ofthe compounds was evaluated using LPSEc (Lipopolysaccharide from E. Coli) stimulated RAW 264.7 macrophage cells. The effect of BHPT compounds on the expressions of cytokines were determined using multi-analyte ELISA kit. The compounds significantly inhibited nitrite production in LPSEc stimulated RAW 264.7 cells with ICso (the concentration of compounds that inhibit nitrite production by 50%) values ranging between 20- 35 µM. BHPT05 is the most potent and it reversed the upregulated pro-inflammatory cytokines and downregulated anti inflammatory cytokines. The metabolic stability ofBHPT05 was determined using mouse, rat, and human liver microsomes and it found to be metabolically stable.en_US
dc.identifier.uri${dspace.baseUrl}/xmlui/handle/1234.56789/2081
dc.identifier.urihttps://hdl.handle.net/20.500.14377/32123
dc.language.isoenen_US
dc.publisherInternational Medical Universityen_US
dc.subjectCytokinesen_US
dc.subjectHydrazonesen_US
dc.subjectThiazolesen_US
dc.subjectAnticonvulsantsen_US
dc.subjectAnalgesicsen_US
dc.subjectMicrosomes, Liveren_US
dc.titleSYNTHESIS OF NEW BENZYLIDENEHYDRAZINYLPHENYLTHIAZOLES AND EVALUATION OF THEIR ANTIINFLAMMATORY ACTIVITY IN VITRO AND METABOLIC STABILITYen_US
dc.typeThesis
dspace.entity.typePublication
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