leachianone G

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 黄酮类化合物
• 英文名称: leachianone G
• 英文别名: 2’,4’,5,7-tetrahydroxy-8-prenylflavanone；(+/-)-Leachianone G；2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-8-(3-methylbut-2-enyl)-2,3-dihydrochromen-4-one
• 化学式: C₂₀H₂₀O₆
• 分子量: 356.375
• InChiKey: VBOYLFNGTSLAAZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  107
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-[2,4-Bis(methoxymethoxy)phenyl]-5,7-bis(methoxymethoxy)-8-(3-methylbut-2-enyl)-2,3-dihydrochromen-4-one 在 盐酸 、 甲醇 作用下， 以 四氢呋喃 为溶剂， 生成 leachianone G
  参考文献：
  名称：

  Synthesis, biological evaluation of prenylflavonoids as vasorelaxant and neuroprotective agents

  摘要：

  A series of prenylflavonoids with multiple hydroxyl groups were synthesized and evaluated for their vasorelaxant activities against rat aorta rings pre-contracted by phenylephrine (PE), as well as their neuroprotective effects against OGD induced PC12 cell injury. The results indicated that the prenyl group at A-ring of prenylflavonoids, as well as hydroxyl groups at B-ring was important for their activities. (+/-)Leachianone G 1b, bearing 8-prenyl and 2',4'-dihydoxyl groups, exhibited the most potent vasorelaxant and neuroprotective effects. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.04.120

文献信息

• T-TYPE CALCIUM CHANNEL INHIBITOR
  申请人：KINKI UNIVERSITY

  公开号：US20200308132A1

  公开（公告）日：2020-10-01

  A new analgesic has been developed for T-type calcium channels as therapeutic targets. The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1): wherein each of R 1 and R 2 independently represents —H or —OH; R 3 represents —OH; R 4 represents —OH or —H; R 5 represents a straight or branched alkyl or cycloalkyl-alkyl group having one to ten carbon atoms or a straight or branched alkenyl or cycloalkyl-alkenyl group having two to ten carbon atoms, or a pharmaceutically acceptable salt or solvate thereof. The present invention also provides this T-type calcium channel inhibitor, a medicament containing the T-type calcium channel inhibitor, and a therapeutic or prophylactic agent for a disease having an effective T-type calcium channel inhibitory action.

  已经开发出一种新的镇痛剂，用于T型钙通道作为治疗靶点。本发明提供了一种T型钙通道抑制剂，其化学式表示为（1）：其中R1和R2分别独立表示—H或—OH；R3表示—OH；R4表示—OH或—H；R5表示具有一到十个碳原子的直链或支链烷基或环烷基烷基，或具有两到十个碳原子的直链或支链烯基或环烷基烯基，或其药学上可接受的盐或溶剂。本发明还提供了这种T型钙通道抑制剂，含有T型钙通道抑制剂的药物，以及用于具有有效T型钙通道抑制作用的疾病的治疗或预防剂。
• T-type calcium channel inhibitor
  申请人：KINKI UNIVERSITY

  公开号：US10633358B2

  公开（公告）日：2020-04-28

  The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1), a pharmaceutically acceptable salt of this compound or a solvate of this compound. The present invention also provides: this T-type calcium channel inhibitor; a pharmaceutical product containing this T-type calcium channel inhibitor; and a therapeutic agent or prophylactic agent for diseases, the effective action of which is a T-type calcium channel inhibitory action. (In formula (1), each of R1 and R2 independently represents H, —OH or —OR11 wherein R11 represents a C1-3 alkyl group; each of R3 and R4 independently represents H, —OH or —OR12, wherein R12 represents a C1-3 alkyl group; and each of R5 and R6 independently represents H, a halogen atom, a C1-10 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a phenyl group (which may be substituted by a C1-6 alkoxy group or a halogen atom), a —C1-3 alkyl-phenyl group (which may be substituted by a C1-6 alkyloxy group or a halogen atom) or a C10-50 prenyl group.)

  本发明提供了一种 T 型钙通道抑制剂，它是由式（1）代表的化合物、该化合物的药学上可接受的盐或该化合物的溶液。本发明还提供：这种 T 型钙通道抑制剂；含有这种 T 型钙通道抑制剂的药品；以及一种治疗剂或疾病预防剂，其有效作用为 T 型钙通道抑制作用。式（1）中，R1 和 R2 各自独立地代表 H、-OH 或-OR11，其中 R11 代表 C1-3 烷基；R3 和 R4 各自独立地代表 H、-OH 或-OR12，其中 R12 代表 C1-3 烷基；R5和R6各自独立地代表H、卤素原子、C1-10烷基、C2-6烯基、C2-6炔基、苯基（可被C1-6烷氧基或卤素原子取代）、-C1-3烷基苯基（可被C1-6烷氧基或卤素原子取代）或C10-50链烯基。)
• US11517556B2
  申请人：GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGY

  公开号：US11517556B2

  公开（公告）日：2022-12-06

  The present invention relates to novel compounds capable of activating BKCa channels. The use of a composition of the present invention can effectively activate the BKCa channels, and can be used for prevention or treatment of various diseases caused by the deactivation of BKCa channels or the degradation of BKCa channel activity.

  本发明涉及能够激活 BKCa 通道的新型化合物。使用本发明的组合物可以有效激活 BKCa 通道，并可用于预防或治疗因 BKCa 通道失活或 BKCa 通道活性降低而引起的各种疾病。
• EXTRAKTE AUS SOPHORA-ARTEN, VERFAHREN ZU IHRER HERSTELLUNG UND VERWENDUNG
  申请人：Dr. Willmar Schwabe GmbH & Co. KG

  公开号：EP1294388B1

  公开（公告）日：2004-01-07
• EP3000465B1
  申请人：——

  公开号：EP3000465B1

  公开（公告）日：2021-03-31