期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 134, 期 41, 页码 17320-17332出版社
AMER CHEMICAL SOC
DOI: 10.1021/ja308429f
关键词
-
资金
- National Institute of Health (U.S.A.) [AI055475, CA100101, R01 AI090141]
- Fonds de Recherche Quebec
- Bristol-Myers Squibb
- Skaggs Research Institute
- Division of Microbiology and Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institute of Health (U.S.A.), Department of Health and Human Services [HHSN272201100019I/HHSN27200001/B01]
An improved sulfenylation method for the preparation of epidithio-, epitetrathio-, and bis-(methylthio)diketopiperazines from diketopiperazines has been developed. Employing NaHMDS and related bases and elemental sulfur or bis[bis(trimethylsilyl)amino]trisulfide (23) in THF, the developed method was applied to the synthesis of a series of natural and designed molecules, including epicoccin G (1), 8,8'-epi-ent-rostratin B (2), gliotoxin (3), gliotoxin G (4), emethallicin E (5), and haematocin (6). Biological screening of selected synthesized compounds led to the discovery of a number of nanomolar antipoliovirus agents (i.e., 46, 2,2'-epi-46, and 61) and several low-micromolar anti-Plasmodium falciparum lead compounds (i.e., 46, 2,2'-epi-46, 58, 61, and 1).
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据