广木香醇衍生物的合成及其对幽门螺杆菌的抗菌活性。

Synthesis of plaunotol derivatives and their antibacterial activities against Helicobacter pylori.

作者信息

Tago K, Minami E, Masuda K, Akiyama T, Kogen H

机构信息

Exploratory Chemistry Research Laboratories, Sankyo Co., Ltd, 1-2-58, Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.

出版信息

Bioorg Med Chem. 2001 Jul;9(7):1781-91. doi: 10.1016/s0968-0896(01)00080-3.

DOI:10.1016/s0968-0896(01)00080-3

PMID:11425580

Abstract

Plaunotol, a known antiulcer drug, has antibacterial activities against Helicobacter pylori. Plaunotol thiourea derivatives 2--4 and diol derivatives 6--10 were designed in search for a compound with high antibacterial activities. Thiourea derivatives 2--4 were synthesized regioselectively using our effective synthetic route for plaunotol (1), and diol derivatives 6--10 were also synthesized. Their antibacterial activities against H. pylori are described and we found that the most potent antibacterial agent was C1-thiourea derivative 2c.

摘要

已知的抗溃疡药物紫苏醇对幽门螺杆菌具有抗菌活性。设计了紫苏醇硫脲衍生物2 - 4和二醇衍生物6 - 10，以寻找具有高抗菌活性的化合物。硫脲衍生物2 - 4通过我们有效的紫苏醇（1）合成路线进行区域选择性合成，二醇衍生物6 - 10也已合成。描述了它们对幽门螺杆菌的抗菌活性，我们发现最有效的抗菌剂是C1 - 硫脲衍生物2c。