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SYNTHESIS OF SOME PIPERIDINE DERIVATIVES HAVING POTENTIAL BIOLOGICAL ACTIVITIES

Source: OAI

ABSTRACT Piperidines are very important compounds because of their presence in numerous alkaloids, pharmaceuticals, agrochemical and as synthetic intermediates. Biologically active alkaloids of the substituted piperidine ring system have been targeted for their total or partial synthesis. Synthetic efforts were also made fro modifications of pethidine and morphine like compounds, which led to the synthesis of new opiate having agonist as well as antagonistic activities. In many families of opiate narcotic analgesics small variations in chemical structures have changed the extent to which an analogue exhibits agonist and antagonist activity During the course of present work several alkyl/acyl/sulfonyl/benzoyl-aryl derivatives of 4-methylpiperidine were synthesized in order to evaluate their biological effects. The resulting derivatives were screened for brine shrimp lethality (cytotoxic) phytotoxic antibacterial, antifungal, insecticidal, urease inhibition and analgesic activities. The structure of all newly synthesized compounds was confirmed by CHN analysis and their melting points. Amongst the compounds showed good cytotoxic activity, whereas in lemna welv phytotoxic bioassay few compounds showed 100% of activity at high concentration i.e. 100% against all grain pests used in this test. Nevertheless in urease inhibition bioassay few compounds showed good activities. Antinoceceptive effects of these compounds were examined with the acetic acid induced abdominal contraction test (writhing test) and formalin induced paw licking response in mice. In writhing test compounds showed varying degree of activities. Similarly in formalin induced paw licking response compounds showed moderate to less activity in first and second phases

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