新型含morpholin硫酸酐的合成及生物活性研究

I.N. Anuarbekova, Ye.S. Sychyeva, D.B. Markina, M.S. Mukanova
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引用次数: 0

摘要

啉是一种很有前途的多功能六元杂环化合物,是一种广受欢迎的具有广泛生物学和药理活性的药效团。本工作的目的是合成具有生物活性的化合物,以3-morpholinepropylamine为基础,测定所合成化合物的结构和生物活性。结果和讨论。以3-形态聚丙基氨基硫代酸钠与相应酸的氯化物进行酰化反应,合成了乙酸、丙酸、苯甲酸、4-氯苯甲酸和2,4-二氯苯甲酸3-聚丙基氨基硫代酸乙酯。在丙酮中进行了2 ~ 3 h的室温合成。根据元素分析数据、红外光谱、1Н和13С核磁共振波谱确定了合成化合物的结构。结论。通过实验室和田间试验发现,使用异丙基氨基硫代硫酸酐有助于增加小麦和云杉的种芽形成。0.01%浓度的丙酸3-morpholinopropylcarbamothioic硫酸酐能使小麦种子的苗长达到5.1 cm,芽发芽率提高88%;云杉种子的苗长达到7.3 cm,芽发芽率分别比对照(4.4 cm、86%和4.0 cm、84%)高87%。苯甲酸(3-morpholinopropyl)氨基硫酸酐在0.01%的浓度下表现出较强的成芽能力,剪后绣线菊的枝长平均为3.91 cm,高于对照(1.63 cm),高于Kornevin (2.58 cm)和KN-2 (3.59 cm)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
SYNTHESIS AND BIOLOGICAL ACTIVITY OF NEW MORPHOLIN-CONTAINING THIOANHYDRIDES
Morpholine is a promising and versatile six-membered heterocycle, a popular pharmacophore with a wide spectrum of biological and pharmacological activity. The purpose of this work is the synthesis of biologically active compounds, based on 3-morpholinepropylamine, the determination of the structure and biological activity of the synthesized compounds. Results and discussion. Acetic, propionic, benzoic, 4-chlorobenzoic and 2,4-dichlorobenzoic 3-morpholinopropylcarbamothioic thioanhydrides have been synthesized as a result of acylation of sodium 3-morpholylpropylcarbadithioate with the corresponding acid’s chlorides. The synthesis has been carried out in acetone at the room temperature for 2 – 3 h. The structure of the synthesized compounds has been established on the basis of the elemental analysis data, IR spectra, 1Н and 13С NMR spectroscopy. Conclusion. As a result of the laboratory and field tests, it has been found that the use of morpholinopropylcarbamothioic thioanhydrides contribute to an increase in the seed shoot formation of wheat and spruce. Propionic 3-morpholinopropylcarbamothioic thioanhydride activates at a concentration of 0.01% the seedlings length of wheat seeds up to 5.1 cm and increases the germination of shoots up to 88%, and on spruce seeds, the seedlings length is 7.3 cm and the germination of shoots is 87% as compared with the control (4.4 cm, 86% and 4.0 cm, 84%), respectively. Benzoic (3-morpholinopropyl)carbamothioic thioanhydride has shown at a concentration of 0.01% a high shoot-forming ability, the length of shoots by cutting Spiraea Vanhouttei is on average 3.91 cm, as compared with the control (1.63 cm) and with the preparations Kornevin (2.58 cm) and KN-2 (3.59 cm).
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