• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Cogent Chemistry >Small-molecule inhibitors of the tuberculosis target, phenylalanyl-tRNA synthetase from Penicillium griseofulvum CPCC-400528
【24h】

Small-molecule inhibitors of the tuberculosis target, phenylalanyl-tRNA synthetase from Penicillium griseofulvum CPCC-400528

机译：结核病靶标的小分子抑制剂，灰霉青霉CPCC-400528的苯丙氨酰-tRNA合成酶

获取原文
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Phenylalanyl-tRNA synthetase (PheRS), a member of aminoacyl-tRNA synthetase family, was the new target of anti-tubercular drug discovery. In an attempt to fully exploit the new potential anti-tuberculosis drugs presented in micro-organisms, we developed a high-throughput screening assay against Mycobacterium tuberculosis (Mtb ) PheRS and then screened a library consisting of 32,000 strains and 1500 natural product-derived compounds. One potent hit extract of Penicillium griseofulvum CPCC-400528 was identified. In this study, isopatulin (1), (+)-epiepoformin (2) and gentisyl alcohol (3), three patulin-producing intermediates, together with three indole-tetramic acids, α-cyclopiazonic acid (4), β-cyclopiazonic acid (5) and iso-α-cyclopiazonic acid (6), were isolated and identified as bioactive constituents from P. griseofulvum CPCC-400528. Their structures were elucidated on the basis of spectroscopic data. Compounds 1, 3, 4, and 5 exhibited Mtb PheRS-inhibiting activities, as well as moderate to weak anti-tuberculosis activities against Mtb H37Rv.
机译：苯丙氨酰-tRNA合成酶（PheRS）是氨酰基-tRNA合成酶家族的成员，是抗结核药物发现的新目标。为了充分利用微生物中潜在的新型抗结核药物，我们开发了针对结核分枝杆菌（Mtb）PheRS的高通量筛选测定方法，然后筛选了由32,000株和1500种天然产物来源的化合物。鉴定出一种有效的灰霉菌青霉菌CPCC-400528的有效提取物。在这项研究中，异patulin（1），（+）-epipoformin（2）和龙胆醇（3），三种产生棒曲霉素的中间体，以及三种吲哚-四酸，α-环吡嗪酸（4），β-环吡嗪酸分离出（5）和异-α-环吡嗪酸（6），并将其鉴定为来自iP的生物活性成分。灰褐色CPCC-400528。根据光谱数据阐明了它们的结构。化合物1、3、4和5表现出Mtb PheRS抑制活性，以及​​针对Mtb H37Rv的中度至弱抗结核活性。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号