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Synthesis, Characterization and Anti Inflammatory activity of some novel 5-((6-(methylthio)benzo[d]oxazol-2-yl)methyl)-3-((4-substituted piperazin-1-yl)methyl)-1,3,4-oxadiazole-2(3H)-thione derivatives
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| Author:
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T.PRATHIMA , T.RAMAMOHAN REDDY
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| Abstract:
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The design, synthesis, spectral and biological activities of some new benzo[d]oxazole derivatives are studied in this work. The acid hydrazides 2-(6-(methylthio)-benzo[d]oxazol-2-yl) acetohydrazide (II) was subjected to cyclization with carbon disulphide under basic conditions to yield 5-((6-(methylthio)-benzo[d]oxazol-2-yl) methyl)-1,3,4-oxadiazole-2(3H)-thione (III) which on aminomethylation with formaldehyde and substituted1-phenylpiperazine afforded a series of Mannich bases (P1-P15). Purity of the compounds has been confirmed by TLC. The structures of these newly synthesized compounds were established on the basis of their IR, 1H-NMR, and Mass spectral data. All the title compounds have been screened for their anti-inflammatory activity. It's worth noting that title compounds (P1-P15) were shown to have anti-inflammatory efficacy as compared to the normal medication, diclofenac at 10 mg/kg p.o, in a carrageenin-induced paw oedema test in rats. The tested compounds showed anti-inflammatory activity ranging from 26.23 % (P7) to 75.63 % (P13) whereas standard drug diclofenac sodium showed 73.66 % inhibition after 3h. The highest activity (78.71 %) was found for the Mannich base, P13.
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| Keyword:
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benzo[d]oxazole, Anti-inflammatory, paw edema
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| EOI:
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-
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| DOI:
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https://doi.org/10.31838/ijpr/2020.12.03.530
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| Download:
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