5-[[3-(1-phenylethoxy)-4-(2-phenylethoxy)phenyl]metheno]-4-oxo-2-thioxo-3-thiazolidineacetic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 5-[[3-(1-phenylethoxy)-4-(2-phenylethoxy)phenyl]metheno]-4-oxo-2-thioxo-3-thiazolidineacetic acid
• 英文别名: 5-[[[3-(1-phenylethoxy)-4-(2-phenylethoxy)]phenyl]methylene]-4-oxo-2-thioxo-3-thiazolidineacetic acid；2-Thioxo-4-oxo-5-[3-[(alpha-methylbenzyl)oxy]-4-(phenethyloxy)benzylidene]thiazolidine-3-acetic acid；2-[(5Z)-4-oxo-5-[[3-(1-phenylethoxy)-4-(2-phenylethoxy)phenyl]methylidene]-2-sulfanylidene-1,3-thiazolidin-3-yl]acetic acid
• 化学式: C₂₈H₂₅NO₅S₂
• 分子量: 519.642
• InChiKey: FFYJVTLTZYPAAB-UQQQWYQISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.4
• 重原子数：
  36
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  134
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  3-羧甲基绕丹宁 、 3-(1-Phenylethoxy)-4-(2-phenylethoxy)-benzaldehyde 生成 5-[[3-(1-phenylethoxy)-4-(2-phenylethoxy)phenyl]metheno]-4-oxo-2-thioxo-3-thiazolidineacetic acid
  参考文献：
  名称：

  Rhodanine-3-acetic acid derivatives as inhibitors of fungal protein mannosyl transferase 1 (PMT1)

  摘要：

  The first inhibitors of fungal protein: mannosyl transferase 1 (PMT1) are described. They are based upon rhodanine-3-acetic acid and several compounds have been identified, for example, 5-[[3-(1-phenylethoxy)-4-(2-phenylethoxy)phenyl]methylene]4-oxo-2-thioxo-3-thiazolidineacetic acid (5a), which inhibit Candida albicans PMT1 with IC(50)s in the range 0.2-0.5 muM. Members of the series are effective in inducing changes in morphology of C. albicans in vitro that have previously been associated with loss of the transferase activity. These compounds could serve as useful tools for studying the effects of protein O-mannosylation and its relevance in the search for novel antifungal agents. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.05.050

文献信息

• HIGH SECRETION PRODUCTION METHOD OF PROTEIN
  申请人：Kirin Pharma Kabushiki Kaisha

  公开号：EP2022855A1

  公开（公告）日：2009-02-11

  This invention provides a means for enabling high-level secretory production of proteins, in particular proteins having complicated structures such as antibodies, in host cells such as yeast cells. The invention also provides transformed yeast cells having the activated HAC1 gene and the RRBP1 gene and a method for enabling high-level secretory production of foreign proteins using such transformed host cells by inhibiting O-sugar chain formation indigenous to host cells such as yeast cells.

  本发明提供了一种在宿主细胞（如酵母细胞）中高水平分泌生产蛋白质，特别是具有复杂结构的蛋白质（如抗体）的方法。本发明还提供了具有活化的 HAC1 基因和 RRBP1 基因的转化酵母细胞，以及通过抑制酵母细胞等宿主细胞本地的 O-糖链形成，利用这种转化宿主细胞实现高水平分泌性生产外来蛋白质的方法。
• METHOD FOR HIGH-LEVEL SECRETION AND PRODUCTION OF PROTEIN
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2210940A1

  公开（公告）日：2010-07-28

  This invention provides a means for high-level secretory production of a protein, and, in particular, a protein having a complicated structure such as an antibody, in a host cell such as a yeast cell. This invention provides a method for high-level secretory production of a foreign protein with the use of a transformed host cell having one or more types of chaperone protein genes and via suppression of O sugar chain inherent to a host cell such as a yeast cell.

  本发明提供了一种在酵母细胞等宿主细胞中高水平分泌生产蛋白质，特别是具有复杂结构的蛋白质（如抗体）的方法。本发明提供了一种利用具有一种或多种伴侣蛋白基因的转化宿主细胞，通过抑制酵母细胞等宿主细胞固有的 O 糖链，高水平分泌生产外来蛋白质的方法。
• METHOD FOR IMPROVED HIGH SECRETORY PRODUCTION OF PROTEINS
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP3196304A1

  公开（公告）日：2017-07-26

  The object of the present invention is to provide a production system that is capable of high-level secretory production of a protein (and in particular, a protein with a complicated structure such as a structure with S-S bonds) in a host cell such as yeast and is suitable for industrial production with high safety that does not require explosion-proof facilities. The present invention provides a transformed yeast into which a chaperone gene has been introduced and in which the aox1 gene and/or the protease gene have been disrupted and a method for producing a protein involving the use of such transformed yeast.

  本发明的目的是提供一种生产系统，该系统能够在酵母等宿主细胞中高水平地分泌生产蛋白质（特别是具有复杂结构的蛋白质，如具有S-S键的结构），并适用于不需要防爆设施的高安全性工业生产。本发明提供了一种引入了伴侣蛋白基因并破坏了 aox1 基因和/或蛋白酶基因的转化酵母，以及一种使用这种转化酵母生产蛋白质的方法。
• BENZYLIDENE THIAZOLIDINEDIONES AND THEIR USE AS ANTIMYCOTIC AGENTS
  申请人：UCB, S.A.

  公开号：EP1313471B1

  公开（公告）日：2007-04-11
• EP3196304B1
  申请人：——

  公开号：EP3196304B1

  公开（公告）日：2021-10-06