2,4-Diamino-5-(4-acetamido-3,5-dichlorobenzyl)-pyrimidine | 62909-65-3

• 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: 2,4-Diamino-5-(4-acetamido-3,5-dichlorobenzyl)-pyrimidine
• 英文别名: N-[2,6-dichloro-4-[(2,4-diaminopyrimidin-5-yl)methyl]phenyl]acetamide
• CAS: 62909-65-3
• 化学式: C₁₃H₁₃Cl₂N₅O
• 分子量: 326.185
• InChiKey: PZHDGKOHZZQPEH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  107
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  盐酸胍 、 3-(苯氨基)丙腈 、 N-(2,6-二氯-4-甲酰基苯基)乙酰胺 在 sodium ethanolate 、 sodium 作用下， 以 乙醇 为溶剂， 生成 2,4-Diamino-5-(4-acetamido-3,5-dichlorobenzyl)-pyrimidine
  参考文献：
  名称：

  2,4-Diamino-5-benzylpyrimidines

  摘要：

  本发明提供了由式##STR1##所表示的2,4-二氨基-5-苄基嘧啶，其中R.sub.1是H或低碳基；R.sub.2是H，低碳基或R.sub.3 CO-，其中R.sub.3是H，烷基或环烷基-低碳基；X是卤素；以及它们的酸加成盐。这些嘧啶化合物可用作抗菌剂，并作为磺胺类抗菌活性的增强剂。

  公开号：

  US04008236A1

文献信息

• 2,4-Diamino-5-benzylpyrimidines
  申请人：Abbott Laboratories

  公开号：US04008236A1

  公开（公告）日：1977-02-15

  This invention provides 2,4-diamino-5-benzylpyrimidines represented by the formula ##STR1## wherein R.sub.1 is H or loweralkyl; R.sub.2 is H, loweralkyl or R.sub.3 CO-- wherein R.sub.3 is H, alkyl, or cycloalkyl-loweralkyl; and X is a halogen; and the acid addition salts thereof. These pyrimidine compounds are useful as antibacterial agents, and as potentiators of the antibacterial activity of sulfonamides.

  本发明提供了由式##STR1##所表示的2,4-二氨基-5-苄基嘧啶，其中R.sub.1是H或低碳基；R.sub.2是H，低碳基或R.sub.3 CO-，其中R.sub.3是H，烷基或环烷基-低碳基；X是卤素；以及它们的酸加成盐。这些嘧啶化合物可用作抗菌剂，并作为磺胺类抗菌活性的增强剂。
• Combination therapy effective against microorganisms, including drug resistant microorganisms
  申请人：Fleurir ABX LLC

  公开号：US10898501B2

  公开（公告）日：2021-01-26

  Novel antimicrobial compositions comprise at least a form of a fosfomycin (or suitable analogs, or derivatives thereof), and at least one sulfonamide (or suitable analogs, or derivatives thereof), and/or at least one diaminopyridine (or suitable analogs, or derivatives thereof). Said antimicrobial compositions generally include two or more of said components as a novel combination, provided in a single combination or formulation, or provided independently with overlapping exposures of the two or more components. These novel compositions, when provided as the two or more components, are effective against susceptible microorganisms, and are effective against susceptible drug-resistant microorganisms (e.g., bacteria, parasites), including multi-drug resistant bacteria. These novel compositions are also effective against microorganisms or strains thereof now susceptible to the combination even though said microorganisms or strains thereof were previously found or were considered resistant or intolerant to at least one of the components of the novel composition, when the at least one component was used alone at what was considered an effective dosing amount or concentration.

  新型抗菌组合物至少包括一种形式的磷霉素（或合适的类似物，或其衍生物）和至少一种磺酰胺（或合适的类似物，或其衍生物），和/或至少一种二氨基吡啶（或合适的类似物，或其衍生物）。所述抗菌组合物一般包括两种或两种以上所述成分的新型组合，以单一组合或制剂提供，或以两种或两种以上成分的重叠暴露独立提供。这些新型组合物在作为两种或多种成分提供时，对易感微生物有效，对易感耐药微生物（如细菌、寄生虫）有效，包括耐多药细菌。这些新型组合物对现在对组合物易感的微生物或菌株也有效，即使所述微生物或菌株以前被发现或被认为对新型组合物的至少一种成分具有抗药性或不耐受性，当至少一种成分以被认为有效的剂量或浓度单独使用时也是如此。
• COMBINATION THERAPY EFFECTIVE AGAINST MICROORGANISMS, INCLUDING DRUG RESISTANT MICROORGANISMS
  申请人：Fleurir Abx LLC

  公开号：EP3220920A1

  公开（公告）日：2017-09-27
• US4008236A
  申请人：——

  公开号：US4008236A

  公开（公告）日：1977-02-15
• US4087528A
  申请人：——

  公开号：US4087528A

  公开（公告）日：1978-05-02