1,8-Dihydroxy-6-methoxy-3-methyl-4a,9a-dihydroanthracene-9,10-dione

• 分子结构分类: 有机化合物 - 苯类化合物 - 蒽
• 英文名称: 1,8-Dihydroxy-6-methoxy-3-methyl-4a,9a-dihydroanthracene-9,10-dione
• 英文别名: 1,8-dihydroxy-6-methoxy-3-methyl-4a,9a-dihydroanthracene-9,10-dione
• 化学式: C₁₆H₁₄O₅
• 分子量: 286.28
• InChiKey: GDKCLRVMYLLXBX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  21
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  83.8
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] INHIBITORS OF ANTIBIOTIC RESISTANCE MEDIATED BY ARN T<br/>[FR] INHIBITEURS DE RÉSISTANCE AUX ANTIBIOTIQUES MÉDIÉE PAR L'ARN T
  申请人：UNIV DEGLI STUDI ROMA LA SAPIENZA

  公开号：WO2021014422A1

  公开（公告）日：2021-01-28

  The present invention relates to diterpene compounds of general formula (I) capable of contrasting the antibiotic-resistance mediated by the ArnT enzyme, to their use as a medicament, in particular for use as an adjuvant of an antibiotic therapy in the treatment of antibiotic-resistant bacterial infections. The invention relates also to associations of one or more of the compounds of formula (I) with at least another active ingredient, in particular an antibacterial agent and/or an antibiotic, and compositions comprising one or more compounds of formula (I) or the association according to the present invention and at least one pharmaceutically acceptable excipient and/or carrier as well as to products, in particular medical devices, comprising at least a compound, an association or a composition according to the present invention. Moreover, the invention relates to the use of compounds of formula (I) to sensitize a bacterium to an antibacterial agent or an antibiotic, for example, colistin (polymyxin E) or polymyxin B and to an in vivo or in vitro method for sensitizing a bacterium to an antibacterial agent or an antibiotic comprising the exposure of said bacterium to one or more compounds of formula (I) together with colistin.

  本发明涉及通式（I）的二萜化合物，其能够对抗由ArnT酶介导的抗生素耐药性，以及它们作为药物的用途，特别是作为抗生素治疗中的辅助剂，用于治疗抗生素耐药性细菌感染。本发明还涉及将通式（I）的一个或多个化合物与至少另一种活性成分，特别是抗菌剂和/或抗生素，结合在一起的组合物，以及包含一个或多个通式（I）化合物或根据本发明的组合物和至少一种药用可接受的载体和/或载体的组合物，以及包含至少一种化合物、组合物或组合物的产品，特别是医疗器械。此外，本发明涉及使用通式（I）的化合物使细菌对抗菌剂或抗生素敏感化的用途，例如，科利斯汀（多粘菌素E）或多粘菌素B，以及一种体内或体外的方法，用于使细菌对抗菌剂或抗生素敏感化，包括将该细菌暴露于与科利斯汀一起使用的一个或多个通式（I）化合物。
• INHIBITORS OF ANTIBIOTIC RESISTANCE MEDIATED BY ARNT
  申请人：UNIVERSITÀ DEGLI STUDI DI ROMA "LA SAPIENZA"

  公开号：US20220259249A1

  公开（公告）日：2022-08-18

  The present invention relates to diterpene compounds of general formula (I) capable of contrasting the antibiotic-resistance mediated by the ArnT enzyme, to their use as a medicament, in particular for use as an adjuvant of an antibiotic therapy in the treatment of antibiotic-resistant bacterial infections. The invention relates also to associations of one or more of the compounds of formula (I) with at least another active ingredient, in particular an antibacterial agent and/or an antibiotic, and compositions comprising one or more compounds of formula (I) or the association according to the present invention and at least one pharmaceutically acceptable excipient and/or carrier as well as to products, in particular medical devices, comprising at least a compound, an association or a composition according to the present invention. Moreover, the invention relates to the use of compounds of formula (I) to sensitize a bacterium to an antibacterial agent or an antibiotic, for example, colistin (polymyxin E) or polymyxin B and to an in vivo or in vitro method for sensitizing a bacterium to an antibacterial agent or an antibiotic comprising the exposure of said bacterium to one or more compounds of formula (I) together with colistin.