N-(1-naphthyl)-2-thiophenesulfonamide | 53442-47-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: N-(1-naphthyl)-2-thiophenesulfonamide
• 英文别名: N-naphthalen-1-ylthiophene-2-sulfonamide
• CAS: 53442-47-0
• 化学式: C₁₄H₁₁NO₂S₂
• 分子量: 289.4
• InChiKey: QWMMZMCPCHWSCU-UHFFFAOYSA-N

物化性质

• 溶解度：
  5.1 [ug/mL]

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  82.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N-(1-naphthyl)-2-thiophenesulfonamide 、 硫酸二甲酯 、 sodium hydroxide 以70%的产率得到
  参考文献：
  名称：

  EL-MAGHRABY, A. A.;MOHAMED, N. A., J. CHEM. TECHNOL. AND BIOTECHNOL., 1983, 33, N 1, 25-32

  摘要：

  DOI：
• 作为产物：
  描述：

  2-噻吩磺酰氯 、 1-萘胺 、 吡啶 以79%的产率得到
  参考文献：
  名称：

  EL-MAGHRABY, A. A.;MOHAMED, N. A., J. CHEM. TECHNOL. AND BIOTECHNOL., 1983, 33, N 1, 25-32

  摘要：

  DOI：

文献信息

• [EN] PROTEOLYSIS TARGETING CHIMERIC (PROTAC) COMPOUND WITH E3 UBIQUITIN LIGASE BINDING ACTIVITY AND TARGETING ALPHA-SYNUCLEIN PROTEIN FOR TREATING NEURODEGENERATIVE DISEASES<br/>[FR] COMPOSÉ CHIMÈRE CIBLANT LA PROTÉOLYSE (PROTAC) AYANT UNE ACTIVITÉ DE LIAISON À L'UBIQUITINE LIGASE E3 ET CIBLANT UNE PROTÉINE ALPHA-SYNUCLÉINE POUR LE TRAITEMENT DE MALADIES NEURODÉGÉNÉRATIVES
  申请人：ARVINAS OPERATIONS INC

  公开号：WO2020041331A1

  公开（公告）日：2020-02-27

  The present disclosure relates to bifunctional compounds, which find utility as modulators of alpha-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/ inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure. Such diseases or disorders are alpha-synucleinopathies or neurodegenerative diseases associated with alpha-synuclein accumulation and aggregation, such as e.g. Parkinson Disease, Alzheimer's Disease, dementia, dementia with Lewy bodies or multiple system atrophy, in particular Parkinson's Disease.

  本公开涉及双功能化合物，其作为α-突触核蛋白（目标蛋白）的调节剂具有实用性。具体而言，本公开涉及包含一端为Von Hippel-Lindau、cereblon、凋亡抑制蛋白或鼠双分子同源物2配体的双功能化合物，该配体与相应的E3泛素连接酶结合，另一端为与目标蛋白结合的基团，使得目标蛋白靠近泛素连接酶以促使目标蛋白的降解（和抑制）。本公开展示了与目标蛋白的降解/抑制相关的广泛药理活性范围。本公开的化合物和组合物用于治疗或预防由目标蛋白聚集或积累导致的疾病或紊乱。这些疾病或紊乱是与α-突触核蛋白积累和聚集相关的α-突触核蛋白病或神经退行性疾病，例如帕金森病、阿尔茨海默病、痴呆症、带有Lewy小体的痴呆症或多系统萎缩，特别是帕金森病。
• BISSULFONAMIDE DERIVATIVES AS ENZYME INHIBITORS
  申请人：Arrow Therapeutics Limited

  公开号：EP1239852A2

  公开（公告）日：2002-09-18
• NOVEL SULFONAMINOQUINOLINE HEPCIDIN ANTAGONISTS
  申请人：Vifor (International) AG

  公开号：EP2675526A1

  公开（公告）日：2013-12-25
• [EN] ENZYME INHIBITORS<br/>[FR] INHIBITEURS D'ENZYMES
  申请人：ARROW THERAPEUTICS LTD

  公开号：WO2001028537A2

  公开（公告）日：2001-04-26

  Bissulfonamide derivatives of formula (I) are capable of inhibiting: a) the biosynthesis of aromatic amino acids via the shikimate pathway and b) the catabolism of quinic acid, wherein: Ar is an aryl or heteroaryl group; R1 and R2 are the same or different and each represent hydrogen or alkyl or R1 and R2 together form a C1-C3 alkylene group, -CO- or -CS-; and R3 and R4 are the same or different and each represent -alkyl-aryl, -alkyl-heteroaryl, -alkenyl-aryl, -alkenyl-heteroaryl, -alkynyl-aryl-alkynyl-heterorayl, aryl or heteroaryl.
• [EN] NOVEL SULFONAMINOQUINOLINE HEPCIDIN ANTAGONISTS<br/>[FR] NOUVEAUX ANTAGONISTES DE SULFONAMINOQUINOLINE-HEPCIDINE
  申请人：VIFOR INT AG

  公开号：WO2012110603A1

  公开（公告）日：2012-08-23

  The present invention relates to novel hepcidin antagonists of formula (I), pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anaemias, in particular anaemias in connection with chronic inflammatory diseases (ACD: anaemia of chronic disease and Al; anaemia of inflammation).