5-(2-thiophenyl)hydantoin | 74126-04-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: 5-(2-thiophenyl)hydantoin
• 英文别名: DL-5-(2-thienyl)hydantoin；5-(thien-2-yl)hydantoin；5-(2-thienyl)hydantoin；5-thiophen-2-ylimidazolidine-2,4-dione
• CAS: 74126-04-8
• 化学式: C₇H₆N₂O₂S
• 分子量: 182.203
• InChiKey: XQZQMAOUAIJWOX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  86.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-(2-thiophenyl)hydantoin 以 水 为溶剂， 生成 N-carbamyl-D-(-)2-thienylglycine
  参考文献：
  名称：

  Shimizu, Sakayu; Shimada, Hiroaki; Takahashi, Satomi, Agricultural and Biological Chemistry, 1980, vol. 44, # 9, p. 2233 - 2234

  摘要：

  DOI：
• 作为产物：
  描述：

  噻吩 生成 5-(2-thiophenyl)hydantoin
  参考文献：
  名称：

  CHRISTIDIS, Y.

  摘要：

  DOI：

文献信息

• Inhibitors Of Beta-Secretase
  申请人：Dillard Lawrence W.

  公开号：US20110218192A1

  公开（公告）日：2011-09-08

  The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.

  本发明涉及以下结构式所表示的化合物或其药学上可接受的盐。还描述了包含由结构式（I）所表示的化合物的药物组合物和使用这些化合物抑制需要此类治疗的受体中的BACE活性的方法。
• INHIBITORS OF BETA-SECRETASE
  申请人：Dillard Lawrence W.

  公开号：US20130317014A1

  公开（公告）日：2013-11-28

  The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.

  本发明涉及以下结构式所代表的化合物：或其药学上可接受的盐。还描述了包括结构式（I）所代表的化合物的药物组合物以及使用这些化合物抑制需要此类治疗的受体中的BACE活性的方法。
• Spiro-furanohydantoin derivatives, process for their preparation and pharmaceutical compositions containing them
  申请人：PFIZER INC.

  公开号：EP0008229A1

  公开（公告）日：1980-02-20

  Spiro-furanohydantoin derivatives of the formula: and pharmaceutically acceptable metal salts wherein R is hydrogen, methyl, fluoro, chloro or bromo and pharmaceutical compositions thereof are aldose reductase inhibitors useful as therapeutic agents for preventing or alleviating chronic diabetic complications such as diabetic cataracts and neuropathy.

  式中 R 为氢、甲基、氟、氯或溴的螺呋喃海因衍生物： 和药学上可接受的金属盐（其中 R 是氢、甲基、氟、氯或溴）及其药物组合物是醛糖还原酶抑制剂，可用作预防或缓解慢性糖尿病并发症（如糖尿病性白内障和神经病变）的治疗剂。
• Process for the production of D-alpha-amino acids
  申请人：ENIRICERCHE S.p.A.

  公开号：EP0677585A1

  公开（公告）日：1995-10-18

  A process is described for the production of D-α-amino acids by the stereospecific conversion of racemic mixtures of 5-substituted hydantoins, where said conversion is carried out in the presence of a microorganism transformed with a plasmid capable of expressing at high levels and without inducers an enzymatic system capable of converting said hydandoins in the corresponding D-α-amino acids. A plasmid is also described comprising the genes which encode said enzymatic system and a microorganism selected from Escherichia coli or Bacillus subtilis transformed with said plasmid. D-α-amino acids are intermediates useful in the preparation of pharmacologically active substances, pesticides and sweeteners.

  描述了一种通过 5-取代的海因外消旋混合物的立体特异性转化生产 D-α-氨基酸的工艺，其中所述转化是在用质粒转化的微生物存在下进行的，该质粒能够高水平表达一种酶系统，该酶系统无需诱导剂即可将所述海因转化为相应的 D-α-氨基酸。 还描述了一种质粒，其中包括编码所述酶系统的基因和用所述质粒转化的大肠杆菌或枯草杆菌中的微生物。 D-α- 氨基酸是用于制备药理活性物质、杀虫剂和甜味剂的中间体。
• Stable mutants of D-N-alpha-carbamylase
  申请人：ENIRICERCHE S.p.A.

  公开号：EP0677584A1

  公开（公告）日：1995-10-18

  The present invention relates to mutants of D-N-α-carbamylase wherein at least one of the cysteines in position 243, 250 and 279 of the amino acid sequence of the wild type enzyme is substituted with a different residue selected from natural amino acids; a recombinant plasmid comprising a nucleotidic sequence which encodes for at least one of the mutants of D-N-α-carbamylase, host microorganisms transformed with said plasmid and a process for the preparation of these mutants by the culture of said microorganisms. The mutants of D-N-α-carbamylase have a higher enzymatic stability than that of the wild type enzyme and are particularly useful in the preparation of D-α-amino acids providing an improvement in the production yields.

  本发明涉及D-N-α-氨基甲酰酶的突变体，其中野生型酶的氨基酸序列的243、250和279位的半胱氨酸中至少有一个被选自天然氨基酸的不同残基取代；重组质粒，其包含编码至少一种D-N-α-氨基甲酰酶突变体的核苷酸序列；用所述质粒转化的宿主微生物；以及通过培养所述微生物制备这些突变体的工艺。 与野生型酶相比，D-N-α-氨基甲酰酶的突变体具有更高的酶稳定性，尤其适用于制备 D-α-氨基酸，可提高产量。