南华大学学报(自然科学版)
南華大學學報(自然科學版)
남화대학학보(자연과학판)
JOURNAL OF NANHUA UNIVERSITY(SCIENCE AND TECHNOLOGY)
2014年
3期
87-91
,共5页
吗啉类化合物%合成%抗抑郁药理模型%抗抑郁活性
嗎啉類化閤物%閤成%抗抑鬱藥理模型%抗抑鬱活性
마람류화합물%합성%항억욱약리모형%항억욱활성
morpholine compounds%synthesis%anti-depression pharmacological model%anti-depressive activity
设计合成了7个未见报道的新型吗啉类化合物,通过IR、NMR、ESI-MS和元素分析对目标化合物结构进行了表征。利用小鼠强迫游泳及悬尾两个抗抑郁药理模型对所合成的化合物进行抗抑郁药理活性筛选,进行了初步的药效评价研究。结果表明这些化合物显示了不同程度的抗抑郁活性,同等剂量下部分化合物的体内抗抑郁作用显著强于空白组,其中芳香环的3位上具有氟取代基的化合物,抗抑郁活性最高,有进一步研究的价值。
設計閤成瞭7箇未見報道的新型嗎啉類化閤物,通過IR、NMR、ESI-MS和元素分析對目標化閤物結構進行瞭錶徵。利用小鼠彊迫遊泳及懸尾兩箇抗抑鬱藥理模型對所閤成的化閤物進行抗抑鬱藥理活性篩選,進行瞭初步的藥效評價研究。結果錶明這些化閤物顯示瞭不同程度的抗抑鬱活性,同等劑量下部分化閤物的體內抗抑鬱作用顯著彊于空白組,其中芳香環的3位上具有氟取代基的化閤物,抗抑鬱活性最高,有進一步研究的價值。
설계합성료7개미견보도적신형마람류화합물,통과IR、NMR、ESI-MS화원소분석대목표화합물결구진행료표정。이용소서강박유영급현미량개항억욱약리모형대소합성적화합물진행항억욱약리활성사선,진행료초보적약효평개연구。결과표명저사화합물현시료불동정도적항억욱활성,동등제량하부분화합물적체내항억욱작용현저강우공백조,기중방향배적3위상구유불취대기적화합물,항억욱활성최고,유진일보연구적개치。
Seven novel morpholine compounds had been designed and synthetized, the structure of target compounds were confirmed by IR,NMR,ESI-MS and elemental analy-sis. All synthetized compounds were tested by forced swimming test and tail suspension test in mice. The result showed that these compounds display anti-depression activity of differ-ent degrees and the anti-depression effect of part of compounds with the same dose was sig-nificantly better than that of the blank group. The compounds containing a fluorinated sub-stituent at the 3-position of aromatic ring exhibited a higher activity than others. Some of them are worth to be studied further.