2-(4-tert-butylthiazol-2-yl)benzoic acid | 1048367-63-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(4-tert-butylthiazol-2-yl)benzoic acid
• 英文别名: 2-(4-tert-butyl-1,3-thiazol-2-yl)benzoic acid
• CAS: 1048367-63-0
• 化学式: C₁₄H₁₅NO₂S
• 分子量: 261.345
• InChiKey: CRUGZJJYOZVRDD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  78.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(4-tert-butylthiazol-2-yl)benzoic acid 在 草酰氯 、 N,N-二甲基甲酰胺 作用下， 以 二氯甲烷 为溶剂， 生成
  参考文献：
  名称：

  Discovery of benzothiazole derivatives as efficacious and enterocyte-specific MTP inhibitors

  摘要：

  A series of triamide derivatives bearing a benzothiazole core is shown to be potent microsomal triglyceride transfer protein (MTP) inhibitors. In order to minimize liver toxicity, these compounds have been optimized to have activity only in the enterocytes and have limited systemic bioavailability. Upon oral administration, selected analogs within this series have been further demonstrated to reduce food intake along with body weight and thereby improve glucose homeostasis and insulin sensitivity in a 28-day mice diet-induced obesity (DIO) model. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.01.044
• 作为产物：
  描述：

  methyl 2-(4-tert-butylthiazol-2-yl)benzoate 在 乙酸乙酯 、 Brine 、 Sodium sulfate-III 作用下， 以 盐酸 为溶剂， 反应 12.0h， 以to afford 2-(4-tert-butylthiazol-2-yl)benzoic acid as a light yellow solid (280 mg, yield: 92%)的产率得到2-(4-tert-butylthiazol-2-yl)benzoic acid
  参考文献：
  名称：

  Gut microsomal triglyceride transport protein inhibitors

  摘要：

  化学式（I）所代表的化合物是肠道微粒体甘油三酯转移蛋白的抑制剂。这些化合物在治疗糖尿病和肥胖等疾病或病况的患者以及患有这些疾病或病况的风险患者中非常有用。

  公开号：

  US20080249130A1

文献信息

• Gut microsomal triglyceride transport protein inhibitors
  申请人：Vu Chi B.

  公开号：US20080249130A1

  公开（公告）日：2008-10-09

  Compounds represented by formula (I): are inhibitors of gut microsomal triglyceride transfer protein. Such compounds are useful in treating diseases or conditions such as diabetes and obesity, along with patients are risk for developing such diseases or conditions.

  化学式（I）所代表的化合物是肠道微粒体甘油三酯转移蛋白的抑制剂。这些化合物在治疗糖尿病和肥胖等疾病或病况的患者以及患有这些疾病或病况的风险患者中非常有用。
• [EN] GUT MICROSOMAL TRIGLYCERIDE TRANSPORT PROTEIN INHIBITORS<br/>[FR] INHIBITEURS DE PROTÉINES MICROSOMIQUES DE TRANSPORT DES TRIGLYCÉRIDES DE L'INTESTIN
  申请人：SIRTRIS PHARMACEUTICALS INC

  公开号：WO2008100423A1

  公开（公告）日：2008-08-21

  [EN] Compounds represented by formula (I): are inhibitors of gut microsomal triglyceride transfer protein. Such compounds are useful in treating diseases or conditions such as diabetes and obesity, along with patients are risk for developing such diseases or conditions.
  [FR] La présente invention concerne des composés de formule (I), qui sont inhibiteurs de protéine microsomique de transfert des triglycérides de l'intestin. De tels composés sont utiles dans le traitement de maladies ou conditions telles que le diabète et l'obésité, ainsi que des patients à risque de développer de telles maladies ou conditions.
• WO2008/100423
  申请人：——

  公开号：——

  公开（公告）日：——
• Discovery of benzothiazole derivatives as efficacious and enterocyte-specific MTP inhibitors
  作者：Chi B. Vu、Jill C. Milne、David P. Carney、Jeffrey Song、Wendy Choy、Philip D. Lambert、David J. Gagne、Michael Hirsch、Angela Cote、Meghan Davis、Elden Lainez、Nekeya Meade、Karl Normington、Michael R. Jirousek、Robert B. Perni

  DOI：10.1016/j.bmcl.2009.01.044

  日期：2009.3

  A series of triamide derivatives bearing a benzothiazole core is shown to be potent microsomal triglyceride transfer protein (MTP) inhibitors. In order to minimize liver toxicity, these compounds have been optimized to have activity only in the enterocytes and have limited systemic bioavailability. Upon oral administration, selected analogs within this series have been further demonstrated to reduce food intake along with body weight and thereby improve glucose homeostasis and insulin sensitivity in a 28-day mice diet-induced obesity (DIO) model. (C) 2009 Elsevier Ltd. All rights reserved.