2,6,6-三甲基-双环[3,1,1]庚基-3-(4-芳基-2-噻唑)腙类化合物的合成及其抑菌和抗肿瘤活性研究
收稿日期: 2014-04-26
修回日期: 2014-05-22
网络出版日期: 2014-06-11
基金资助
国家自然科学基金（No. 31170538）、江苏省教育厅优势学科经费（No. 201104015）资助项目.
Synthesis and Antibacterial, Antitumor Activity of 2,6,6-Thrimethyl- bicyclo[3,1,1]heptan-3-(4-aryl-2-thiazoyl)hydrazones
Received date: 2014-04-26
Revised date: 2014-05-22
Online published: 2014-06-11
Supported by
Project supported by the National Natural Science Foundation of China (No. 31170538) and the Forestry Public Sector Research Found of State Forestry Administration of China (No. 201104015)
以α-蒎烯为起始原料，经加成、氧化、缩合制得中间体，继而与α-溴代芳基乙酮在常温下反应合成12个新型2，6，6-三甲基-双环[3，1，1]庚基-3-（4-芳基-2-噻唑）腙类化合物，产率达52.4%～88.9%. 其结构经1H NMR，13C NMR，IR，LC/MS和元素分析进行了确证. 初步生物活性测试结果表明：部分目标化合物具有较好的抑菌活性和一定的抗肿瘤活性.
关键词： 庚基-3-(4-芳基-2-噻唑)腙; 合成; 抑菌活性; 抗肿瘤活性
鲍名凯 , 杨益琴 , 谷文 , 徐徐 , 曹明珍 , 王石发 . 2,6,6-三甲基-双环[3,1,1]庚基-3-(4-芳基-2-噻唑)腙类化合物的合成及其抑菌和抗肿瘤活性研究[J]. 有机化学, 2014 , 34(10) : 2146 -2151 . DOI: 10.6023/cjoc201404049
Twelve new 2,6,6-thrimethyl-bicyclo[3,1,1]heptan-3-(4-aryl-2-thiazoyl)hydrazones were synthesized by using α-pinene as starting material in four steps reaction including addition, oxidation, condensation, and reaction with α-bromo- acetophenone under room temperature. The yields of products were in the range from 52.4% to 88.9%. All synthesized new compounds were confirmed by 1H NMR, 13C NMR, IR, LC/MS spectra and elemental analysis. The preliminary bioassay showed that some of the target compounds exhibited significant antibacterial activity and certain antitumor activity.
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