(5Z)-5-(3,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione | 6325-95-7

• 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: (5Z)-5-(3,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
• 英文别名: (E)-5-(3,4-dimethoxybenzylidene)thiazolidine-2,4-dione；5-[(3,4-Dimethoxyphenyl)methylidene]-1,3-thiazolidine-2,4-dione；(5E)-5-[(3,4-dimethoxyphenyl)methylidene]-1,3-thiazolidine-2,4-dione
• CAS: 6325-95-7
• 化学式: C₁₂H₁₁NO₄S
• mdl: MFCD00442438
• 分子量: 265.29
• InChiKey: ARJGUVIAPHIKLE-UXBLZVDNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.166
• 拓扑面积：
  89.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (5Z)-5-(3,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione 、 尿素 在 盐酸 作用下， 以40%的产率得到7-(3,4-dimethoxyphenyl)-6,7-dihydro-3H,4H-triazolo[4,5-d]pyrimidine-2,5-dione
  参考文献：
  名称：

  Akbari; Mehta; Pathak, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2008, vol. 47, # 3, p. 477 - 480

  摘要：

  DOI：
• 作为产物：
  描述：

  2,4-噻唑烷二酮 、 3,4-二甲氧基苯甲醛 在 sodium acetate 、 溶剂黄146 作用下， 反应 12.0h， 以72%的产率得到(5Z)-5-(3,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
  参考文献：
  名称：

  具有广谱抗菌、MRSA 和拓扑异构酶抑制活性的噻唑烷-2,4-二酮连接环丙沙星衍生物

  摘要：

  摘要 制备了一系列环丙沙星/噻唑烷-2,4-二酮杂化物3a-m，并通过IR、1 HNMR、13 CNMR和元素分析对其进行了鉴定。设计的杂种的抗菌活性结果显示光谱向革兰氏阳性菌转移。它们对金黄色葡萄球菌 ATCC 6538表现出优异的活性，最有效的化合物是 3a、3e、3g、3i、3k、3l 和 3m，其 MIC 分别为 0.02、2.03、0.64、0.35、1.04、0.22 和 0.36 µM，与其母体化合物环丙沙星（MIC：5.49 µM）相比。他们还表现出对MRSA AUMC 261的有趣活性3a、3e 和 3l 显示 MIC 值为 5 nM。观察到对革兰氏阴性菌的活性降低，化合物 3l 对肺炎克雷伯菌 ATCC10031的活性略高，MIC 值为 0. 08 µM。从机理上讲，将噻唑烷-2,4-二酮环掺入环丙沙星保留了其通过抑制金黄色葡萄球菌的拓扑异构酶IV和DNA旋转酶来抑制DNA合成的能力。化合物

  DOI：

  10.1007/s11030-021-10302-7

文献信息

• NOVEL COMPOUND HAVING SKIN-WHITENING, ANTI-OXIDIZING AND PPAR ACTIVITIES AND MEDICAL USE THEREFOR
  申请人：Chung Hae Young

  公开号：US20140023603A1

  公开（公告）日：2014-01-23

  Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPARα and PPARγ activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.

  提供了一种具有美白皮肤、抗氧化和PPAR活性的新化合物及其医疗用途，该化合物具有美白皮肤的活性，可抑制酪氨酸酶，因此适用于用于美白皮肤的药物组合物或化妆品；具有抗氧化活性，因此适用于预防和治疗皮肤老化；具有PPAR活性，特别是PPARα和PPARγ活性，因此适用于用于预防和治疗肥胖、代谢性疾病或心血管疾病的药物组合物或保健食品。
• CHEMICAL COMPOUNDS 251
  申请人：Dakin Leslie

  公开号：US20110218182A1

  公开（公告）日：2011-09-08

  The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.

  该发明涉及化学式(I)的化合物及其盐。在某些实施例中，该发明涉及PIM-1和/或PIM-2以及/或PIM-3蛋白激酶活性或酶功能的抑制剂或调节剂。在更进一步的实施例中，该发明涉及包含本文披露的化合物的药物组合物，以及它们在预防和治疗PIM激酶相关疾病和疾病，特别是癌症中的用途。
• Chemical Compounds 251
  申请人：AstraZeneca AB

  公开号：US20150051185A1

  公开（公告）日：2015-02-19

  The invention relates to chemical compounds of formula I, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.

  本发明涉及公式I的化合物及其盐。在某些实施例中，本发明涉及PIM-1和/或PIM-2，以及/或PIM-3蛋白激酶活性或酶功能的抑制剂或调节剂。在更进一步的实施例中，本发明涉及包含本文所披露的化合物的制药组合物，以及它们在预防和治疗PIM激酶相关的疾病和状况，尤其是癌症方面的应用。
• NOVEL COMPOUND HAVING SKIN-WHITENING, ANTI-OXIDIZING AND PPAR ACTIVITIES AND MEDICAL USE THEREOF
  申请人：Pusan National University Industry-University Cooperation Foundation

  公开号：US20160102065A1

  公开（公告）日：2016-04-14

  Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPARα and PPARγ activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.

  提供了一种具有美白、抗氧化和PPAR活性的新化合物及其医疗用途。该化合物具有抑制酪氨酸酶的美白活性，因此可用于美白药物组合物或化妆品产品；具有抗氧化活性，因此可用于预防和治疗皮肤老化；具有PPAR活性，特别是PPARα和PPARγ活性，因此可用于有效预防和治疗肥胖症、代谢疾病或心血管疾病的药物组合物或保健食品。
• Direct electrochemical synthesis of doped conductive polymers on metal alloys
  申请人：The Boeing Company

  公开号：EP2910668A2

  公开（公告）日：2015-08-26

  This disclosure relates generally to the discovery of improved methods of reducing corrosion on metals and metal alloys without using hexavalent chromium reagents. More particularly, the disclosure relates to preparing corrosion resistant metals using doped conducting polymers such as polyaniline (PANI) on metal alloys such as aluminum alloys.

  本公开内容总体上涉及在不使用六价铬试剂的情况下减少金属和金属合金腐蚀的改进方法的发现。更具体地说，本公开涉及在铝合金等金属合金上使用聚苯胺 (PANI) 等掺杂导电聚合物制备耐腐蚀金属。