2-(4,6-dimethyl-3-oxo-[1,2]thiazolo[5,4-b]pyridin-2-yl)-N-(4-phenylbutan-2-yl)acetamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-(4,6-dimethyl-3-oxo-[1,2]thiazolo[5,4-b]pyridin-2-yl)-N-(4-phenylbutan-2-yl)acetamide
• 化学式: C₂₀H₂₃N₃O₂S
• 分子量: 369.5
• InChiKey: MELALEMOJNUKTD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  87.6
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Use of small molecules for the treatment of clostridium difficile toxicity
  申请人：The Board of Trustees of the Leland Stanford Junior University

  公开号：US10172829B2

  公开（公告）日：2019-01-08

  Disclosed are methods and compositions for reducing toxicity associated with infection by Clostridium difficile by inhibiting Clostridium difficile toxin B (TcdB) and/or toxin A (TcdA). Such compounds include ebselen compounds, namely ebselen and its salts, ebselen functional analogues and ebselen structural analogues, as well as certain amide derivatives. This includes Formula I, e.g. 1-methyl-3-phenylpropylamine, Formula II, e.g., 2,2′-diselane-1,2-diylbis[N-(2,4-difluorophenyl)benzamide]; and Formula III, e.g. 2-(2-methoxy-5-methylphenyl)-1, 2-benzoselenazol-3-one. The present compositions may be comprised in a colon-retentive formulation that increases residence of and/or release of the compound in the area where the infection is active.

  所公开的是通过抑制艰难梭菌毒素B（TcdB）和/或毒素A（TcdA）来降低与艰难梭菌感染相关的毒性的方法和组合物。此类化合物包括依布硒化合物，即依布硒及其盐类、依布硒功能类似物和依布硒结构类似物，以及某些酰胺衍生物。这包括式 I，如 1-甲基-3-苯基丙胺；式 II，如 2，2′-二硒-1，2-二基双[N-（2，4-二氟苯基）苯甲酰胺]；以及式 III，如 2-（2-甲氧基-5-甲基苯基）-1，2-苯并硒唑-3-酮。本组合物可包含在一种结肠保留制剂中，以增加化合物在感染活跃区域的停留和/或释放。
• Dimethylarginine Dimethylaminohydrolase Inhibitors and Methods of Use Thereof
  申请人：University The Board of Trustees of the Leland Stanford Junior

  公开号：US20130224259A1

  公开（公告）日：2013-08-29

  The present disclosure provides DDAH modulators. Thus, the present disclosure provides a method of treating a patient suffering from a disorder characterized by excessive NO production and/or elevated DDAH activity, the method comprising administering to said patient an effective amount of a compound of one of formulae I-X. The present disclosure also provides a pharmaceutical composition comprising a compound of one of formulae I-X.
• USE OF SMALL MOLECULES FOR THE TREATMENT OF CLOSTRIDIUM DIFFICILE TOXICITY
  申请人：The Board of Trustees of the Leland Stanford Junior University

  公开号：US20170128420A1

  公开（公告）日：2017-05-11

  Disclosed are methods and compositions for reducing toxicity associated with infection by Clostridium difficile by inhibiting Clostridium difficile toxin B (TcdB) and/or toxin A (TcdA). Such compounds include ebselen compounds, namely ebselen and its salts, ebselen functional analogues and ebselen structural analogues, as well as certain amide derivatives. This includes Formula I, e.g. 1-methyl-3-phenylpropylamine, Formula II, e.g., 2,2′-diselane-1,2-diylbis[N-(2,4-difluorophenyl)benzamide]; and Formula III, e.g. 2-(2-methoxy-5-methylphenyl)-1, 2-benzoselenazol-3-one. The present compositions may be comprised in a colon-retentive formulation that increases residence of and/or release of the compound in the area where the infection is active.
• US9011882B2
  申请人：——

  公开号：US9011882B2

  公开（公告）日：2015-04-21
• [EN] DIMETHYLARGININE DIMETHYLAMINOHYDROLASE INHIBITORS AND METHODS OF USE THEREOF<br/>[FR] INHIBITEURS DE DIMÉTHYLARGININE DIMÉTHYLAMINOHYDROLASE ET PROCÉDÉS D'UTILISATION ASSOCIÉS
  申请人：UNIV LELAND STANFORD JUNIOR

  公开号：WO2013123033A1

  公开（公告）日：2013-08-22

  The present disclosure provides DDAH modulators. Thus, the present disclosure provides a method of treating a patient suffering from a disorder characterized by excessive NO production and/or elevated DDAH activity, the method comprising administering to said patient an effective amount of a compound of one of formulae I-X. The present disclosure also provides a pharmaceutical composition comprising a compound of one of formulae I-X.