5-氯-2-甲氧基-N-[2-(4-甲基苯基)乙基]苯甲酰胺 | 64353-00-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 5-氯-2-甲氧基-N-[2-(4-甲基苯基)乙基]苯甲酰胺
• 英文名称: 5-chloro-2-methoxy-N-(2-<4-methylphenyl>-ethyl)-benzamide
• 英文别名: Benzamide, 5-chloro-2-methoxy-N-[2-(4-methylphenyl)ethyl]-；5-chloro-2-methoxy-N-[2-(4-methylphenyl)ethyl]benzamide
• CAS: 64353-00-0
• 化学式: C₁₇H₁₈ClNO₂
• 分子量: 303.788
• InChiKey: IKDZYODVOCIJKB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  对甲基苯乙胺 、 5-氯-2-甲氧基苯甲酰氯 在 sodium hydroxide 作用下， 以 丙酮 为溶剂， 反应 2.0h， 以80%的产率得到5-氯-2-甲氧基-N-[2-(4-甲基苯基)乙基]苯甲酰胺
  参考文献：
  名称：

  Receptor binding sites of hypoglycemic sulfonylureas and related [(acylamino)alkyl]benzoic acids

  摘要：

  The blood glucose level lowering activity of [(acylamino)ethyl]benzoic acids, such as p-[2-(5-chloro-2-methoxy-benzamido)ethyl]benzoic acid (HB699, 2), is discussed in terms of binding at putative insulin-releasing receptor sites of pancreatic beta cells. The hypoglycemic potencies found for synthetic analogues of 2 indicate that high hypoglycemic activity is only found when a carboxyl group or a group that is readily oxidized to carboxyl in vivo, such as methyl, is attached to the aromatic ring of the phenethyl group. It is proposed that this carboxyl group is able to bind at the same receptor site as the SO2NHCONH group of the sulfonylurea drugs, such as tolbutamide (3). The role of the benzamide group in 2 was attributed to protein binding.

  DOI：

  10.1021/jm00367a016

文献信息

• Acylamino(alkyl)benzene derivatives and process for preparing them
  申请人：Hoechst Aktiengesellschaft

  公开号：US04158063A1

  公开（公告）日：1979-06-12

  The invention relates to acylamino(alkyl)benzene derivatives of the general formula ##STR1## in which W represents a group which can be converted into a carboxyl group, or an aldehyde group or an oxymethyl group or their derivatives or also a low molecular weight alkyl group, preferably a methyl group, X represents an aromatic or hetero-aromatic ring system, Y represents a single chemical bond or a hydrocarbon bridge, and Z represents hydrogen or one or even several other substituents, To their preparation and to pharmaceutical compositions containing them. The compounds have blood sugar lowering activity and may be used in the therapy of diabetes mellitus.

  该发明涉及通式为##STR1##的酰胺基（烷基）苯衍生物，其中W表示可转化为羧基、醛基或氧甲基基团或它们的衍生物或低分子量烷基，优选为甲基基团，X表示芳香或杂芳环系，Y表示单一化学键或烃桥，Z表示氢或一个或多个其他取代基，以及它们的制备方法和含有它们的制药组合物。这些化合物具有降低血糖活性，并可用于糖尿病治疗中。
• ANTI-INFLAMMATORY COMPOUNDS
  申请人：Meingassner Josef Gottfried

  公开号：US20090227620A1

  公开（公告）日：2009-09-10

  The use of a steroid sulfatase inhibitor in the preparation of a medicament for the treatment of inflammatory diseases.

  使用类固醇硫酸酯酶抑制剂制备治疗炎症性疾病的药物。
• TETRONIC AND TETRAMIC ACIDS
  申请人：Godel Thierry

  公开号：US20080132562A1

  公开（公告）日：2008-06-05

  This invention relates to new tetronic and tetramic acid derivatives with beta-secretase inhibitory activity of formula I: wherein R1, R2, R3, R4, R5, R5′, R6 and R6′ are as defined hereinabove, to processes for their preparation, compositions containing said tetronic and tetramic acid derivatives and their use in the treatment and prevention of diseases modulated by an inhibitor of β-secretase, such as Alzheimer's disease.

  本发明涉及一种新的具有β-分泌酶抑制活性的四元酸和四元酰胺衍生物，其化学式为I：其中R1、R2、R3、R4、R5、R5'、R6和R6'如上所定义，以及其制备过程、含有所述四元酸和四元酰胺衍生物的组合物以及它们在治疗和预防由β-分泌酶抑制剂调节的疾病，如阿尔茨海默病等方面的用途。
• Combination of a Steroid Sulfatase Inhibitor and an Ascomycin
  申请人：Meingassner Josef Gottfried

  公开号：US20080293758A1

  公开（公告）日：2008-11-27

  A combination of a steroid sulfatase inhibitor and an ascomycin, which combination is useful as a pharmaceutical.

  一种类固醇硫酸酯酶抑制剂和曲霉素的组合物，该组合物可用作药物。
• Acylsulfonamides as inhibitors of steroid sulfatase
  申请人：Novartis AG

  公开号：EP2228364A1

  公开（公告）日：2010-09-15

  A compound of formula wherein the substituents are as defined in the specification and their use as pharmaceutical, particularly for treatment of disorders mediated by the action of steroid sulfatase.

  式中的化合物 其中的取代基如说明书中所定义，可用作药物，特别是用于治疗由类固醇硫酸酯酶作用介导的疾病。