6,6'-(4-nitro-1H-pyrazole-3,5-diyl)bis(3-bromopyrazolo[1,5-a]pyrimidin-2(1H)-one)

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并嘧啶类
• 英文名称: 6,6'-(4-nitro-1H-pyrazole-3,5-diyl)bis(3-bromopyrazolo[1,5-a]pyrimidin-2(1H)-one)
• 英文别名: 3-bromo-6-[3-(3-bromo-2-oxo-1H-pyrazolo[1,5-a]pyrimidin-6-yl)-4-nitro-1H-pyrazol-5-yl]-1H-pyrazolo[1,5-a]pyrimidin-2-one
• 化学式: C15H7Br2N9O4
• 分子量: 537.08
• InChiKey: ZXUYYFPIPVTPJS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  30
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  164
• 氢给体数：
  3
• 氢受体数：
  9

文献信息

• [EN] REVERSAL OF FOSFOMYCIN RESISTANCE<br/>[FR] INVERSION DE LA RÉSISTANCE À LA FOSFOMYCINE
  申请人：UNIV PITTSBURGH COMMONWEALTH SYS HIGHER EDUCATION

  公开号：WO2018132547A1

  公开（公告）日：2018-07-19

  Compounds, pharmaceutical compositions, and methods for reversing fosfomycin resistance are disclosed. Embodiments of the disclosed compounds inhibit fosfomycin-inhibiting enzymes. Some embodiments of the compounds are FosA inhibitors. The disclosed pharmaceutical compositions include (i) fosfomycin or a pharmaceutically acceptable salt thereof and (ii) a compound, or a pharmaceutically acceptable salt thereof, which inhibits a fosfomycin-inhibiting enzyme. A method of inhibiting growth of a fosfomycin-resistant bacterium includes contacting the bacterium with (i) fosfomycin or a pharmaceutically acceptable salt thereof and (ii) an effective amount of a disclosed compound or a pharmaceutically acceptable salt thereof.

  本文披露了逆转福磺霉素耐药性的化合物、药物组合物和方法。所述化合物的实施方式抑制福磺霉素抑制酶。其中一些实施方式的化合物是FosA抑制剂。所述的药物组合物包括（i）福磺霉素或其药学上可接受的盐和（ii）一种抑制福磺霉素抑制酶的化合物或其药学上可接受的盐。一种抑制福磺霉素耐药细菌生长的方法包括将细菌与（i）福磺霉素或其药学上可接受的盐和（ii）本文披露的化合物或其药学上可接受的盐的有效量接触。
• Reversal of fosfomycin resistance
  申请人：University of Pittsburgh—Of the Commonwealth System of Higher Education

  公开号：US10980811B2

  公开（公告）日：2021-04-20

  Compounds, pharmaceutical compositions, and methods for reversing fosfomycin resistance are disclosed. Embodiments of the disclosed compounds inhibit fosfomycin-inhibiting enzymes. Some embodiments of the compounds are FosA inhibitors. The disclosed pharmaceutical compositions include (i) fosfomycin or a pharmaceutically acceptable salt thereof and (ii) a compound, or a pharmaceutically acceptable salt thereof, which inhibits a fosfomycin-inhibiting enzyme. A method of inhibiting growth of a fosfomycin-resistant bacterium includes contacting the bacterium with (i) fosfomycin or a pharmaceutically acceptable salt thereof and (ii) an effective amount of a disclosed compound or a pharmaceutically acceptable salt thereof.

  本研究公开了用于逆转磷霉素抗药性的化合物、药物组合物和方法。所公开化合物的实施方案可抑制磷霉素抑制酶。化合物的一些实施方案是 FosA 抑制剂。所公开的药物组合物包括(i)磷霉素或其药学上可接受的盐和(ii)抑制磷霉素抑制酶的化合物或其药学上可接受的盐。抑制耐磷霉素细菌生长的方法包括使细菌与(i)磷霉素或其药学上可接受的盐和(ii)有效量的已公开化合物或其药学上可接受的盐接触。