Investigation of 7-benzylidenenaltrexone derivatives as a novel structural antitrichomonal lead compound
Investigation of 7-benzylidenenaltrexone derivatives as a novel structural antitrichomonal lead compound
复制标题
7-亚苄基醛曲酮衍生物作为新型结构抗滴虫先导化合物的研究
DOI：
10.1016/j.bmcl.2015.06.002
复制
发表时间：
2015
期刊：
影响因子：
--
通讯作者：
H.
中科院分区：
文献类型：
--
作者：
Kutsumura;N.; Nakajima;R.; Koyama;Y.; Miyata;Y.; Saitoh;T.; Yamamoto;N.; Iwata;S.; Fujii;H.; Nagase;H.
我们评价了δ阿片受体（DOR）激动剂和拮抗剂的抗滴虫作用。DOR拮抗剂BNTX（2a）及其衍生物2b-d具有抗滴虫活性，MIC为20-40 μM。此外，通过Knoevenagel缩合反应，发展了一种更有效的BNTX衍生物的合成方法。
We evaluated antitrichomonal effects of δ opioid receptor (DOR) agonists and antagonists. Although all the agonists were inactive, the DOR antagonists BNTX (2a) and its derivatives2b–dshowed antitrichomonal activity with MIC of 20–40 μM. In addition, the development of a more effective synthetic method for the BNTX derivatives was achieved by using the Knoevenagel condensation.