偕胺肟衍生物与局部麻醉,抗结核和抗糖尿病活性

L. Kayukova, U. Jussipbekov, K. Praliyev
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引用次数: 1

摘要

О我们在偕胺肟类新衍生物领域的任务是研制比实际使用的药物具有更高活性和更低毒性的新药物。以下是对偕胺肟类新型止痛药、抗结核和抗糖尿病药物的研究结果。测定了α -氯- α -异硝基丙酮、O -芳基- β -氨基丙胺肟、3-[β -(胡椒-1-基)]乙基-5-芳基-1,2,4-恶二唑的亚氮衍生物的传导、浸润和终末麻醉。其中发现了hit化合物。世界各地都在寻找新的抗结核药物。β -(噻吩啉-1-酰基)和β -(4-甲基哌嗪-1-酰基)丙胺肟的O -芳基化产物的盐和碱在体外抗结核结核分枝杆菌DS、DR和MDR菌株筛选过程中表现出高度活性的竞争性化合物。在β -氨基丙胺肟衍生物系列中,对新型降糖药物进行了探索。发现了具有显著抗糖尿病作用的化合物。获得的最有希望的样品的数据以及对其在动物中的平均毒性剂量的初步评估可用于进一步的体内浸润麻醉条件测试、抗糖尿病特性以及结核病剂量和新治疗方案的制定。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Amidoxime Derivatives with Local Anesthetic, Antitubercular, and Antidiabetic Activity
О ur task in the field of new derivatives of amidoximes was the elaboration for new medication with increased activity and lower toxicity than medications used in practice. Here are the results of the search for new painkillers and antitubercular and antidiabetic drugs in the class of amidoxime derivatives. Nitrous derivatives of α -chloro- α -isonitrosoacetone, O -aroyl- β -aminopropioamidoximes, and 3-[ β -(piper-idine-1-yl)]ethyl-5-aryl-1,2,4-oxadiazoles were tested for conduction, infiltration, and terminal anesthesia. Among them hit compounds were discovered. The search for new anti-TB drugs is executed in the world. Salts and bases of O -aroylation products of β -(thiomorpholin-1-yl) and β -(4-methylpiperazin-1-yl) propioamidoximes during in vitro antitubercular screening for DS, DR, and MDR strains of M. tuberculosis manifest themselves as highly active competitive compounds. In the series of the derivatives of β -aminopropioamidoximes, a search for new antidiabetic drugs was done. The compounds with pronounced antidiabetic properties were revealed. The obtained data of the most promising samples with a preliminary assessment of their average toxic dose in animals can be used in further in vivo testing of infiltration anesthesia conditions, of antidiabetic properties, and at the development of doses and new treatment regimens for TB.
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