SYNTHESIS AND BIOLOGICAL ACTIVITY OF SOME N-AMINOTETRAHYDROPYRIDINES

几种N-二氮杂环戊烷的合成及生物活性测定 氨基四氢吡啶类化合物 主要目标是设计、合成和药理作用。 新型药用重要N-氨基-1，2，3，6-氨基-1，2，3，6- 四氢吡啶衍生物。本文报道了一种新型N-环氧氯丙烷的合成。 使用Tamura使用的方法并在 我们的实验室。叶立德的硼氢化钠还原 几种四氢吡啶类化合物的初步药理试验结果 表现出镇痛和抗炎活性，但没有观察到 毒性，即使在非常高的剂量水平。 我们以前的工作为新的和令人兴奋的研究提供了基础，以便 可以制备与最活跃的类似物相关的一系列化合物， 并重新测试并测定了辛醇-水分配系数。一次 积累了足够的数据，将对所制备的化合物进行 进行结构活性分析，研究电子、空间和空间构型。 取代基的亲脂作用。物理和药理数据 在这项研究中获得的药物将被用于设计具有更多 有益的生物活动。 药理学研究的主要重点将是开发一种 易合成、高效、安全的非甾体抗炎药 用于治疗风湿性疾病，包括风湿性关节炎， 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.