SYNTHESIS AND BIOLOGICAL ACTIVITY OF SOME N-AMINOTETRAHYDROPYRIDINES

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Synthesis and Biological Activity Determinations of Some N- aminotetrahydropyridines The primary objective is the design, synthesis and pharmacological evaluation of novel and medicinally important N-amino-1,2,3,6- tetrahydropyridine derivatives. We reported the synthesis of novel N- iminopyridinium ylides using the method employed by Tamura and modified in our laboratory. Sodium borohydride reduction of the ylides afforded preliminary pharmacological test results of a few tetrahydropyridines that exhibited analgesic and anti-inflammatory activities with no observed toxicity, even at very high dose levels. Our earlier work provides the basis for new and exciting studies so that a series of compounds related to athe most active analogs could be prepared, and retested and the octanol-water partition coefficient determined. Once sufficient data are accumulated, the compounds prepared will be subjected to structure activity analysis to study the electronic, steric and lipophilic effects of substituents. The physical and pharmacological data obtained in this study will then be used to design drugs with more beneficial biological activity. The primary focus of the pharmacological studies will be to develop an easily synthesized, effective and safe nonsteroidal anti-inflammatory agent for the treatment of rheumatic diseases, including rheumatoid arthritis, osteoarthritis, gout and rheumatic fever.