SYNTHESIS AND BIOLOGICAL ACTIVITY OF SOME N-AMINOTETRAHYDROPYRIDINES

几种氮杂环丁烷类化合物的合成及生物活性测定 氨基四氢吡啶 主要目标是设计、合成和药理学 评价新的和医学上重要的N-氨基-1，2，3，6- 四氢吡啶衍生物。 本文报道了N-（2-甲氧基苯基）-N-（2 亚氨基吡啶鎓叶立德，使用Tamura采用的方法并在 我们的实验室 硼氢化钠还原叶立德，得到 一些四氢吡啶的初步药理学试验结果， 表现出镇痛和抗炎活性，没有观察到 毒性，即使在非常高的剂量水平。 我们早期的工作为新的和令人兴奋的研究提供了基础， 可以制备与最具活性的类似物相关的一系列化合物， 重新测试并测定辛醇-水分配系数。 一旦 积累了足够的数据，制备的化合物将受到 结构活性分析，研究电子，空间和 取代基的亲脂作用。 物理和药理学数据 这项研究中获得的结果将用于设计药物， 有益的生物活性。 药理学研究的主要重点是开发一种 一种易于合成、安全有效的非甾体抗炎药 用于治疗风湿性疾病，包括类风湿性关节炎， 骨关节炎痛风和风湿热

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.