Clavulanic acid | 1214871-19-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Clavulanic acid
• 英文别名: 3-(2-Hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
• CAS: 1214871-19-8
• 化学式: C₈H₉NO₅
• 分子量: 199.163
• InChiKey: HZZVJAQRINQKSD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  87.1
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• Hybrid molecules QA, wherein Q is an aminoquinoline and a is an antibiotic or a resistance enzyme inhibitor, their synthesis and their uses as antibacterial agent
  申请人：Sanchez Muriel

  公开号：US20060025327A1

  公开（公告）日：2006-02-02

  Aminoquinoline-antibiotic hybrid compounds in the form of hybrid molecules QA, wherein Q is an aminoquinoline and A is an antibiotic or a resistance enzyme inhibitor, their synthesis and their uses as antibacterial agent. This compound is defined by the general formula (I): Q-(Y 1 ) p —(U) p′ —(Y 2 ) p″ -A  (I) in which Q represents an aminoquinoline, (Y 1 ) p —(U) p′ —(Y 2 ) p″ — is an optional spacer arm and A is an antibiotic, one of its derivatives or precursors, or a resistance enzyme inhibitor. The invention unexpectedly enables the activity of the antibiotic to be improved.

  氨基喹啉-抗生素混合物化合物以混合分子QA的形式存在，其中Q是氨基喹啉，A是抗生素或耐药酶抑制剂，它们的合成及用途作为抗菌剂。该化合物由通用公式(I)定义：Q-(Y1)p—(U)p′—(Y2)p″-A  (I)其中Q代表氨基喹啉，(Y1)p—(U)p′—(Y2)p″—为可选的间隔臂，A是抗生素、其衍生物或前体之一，或耐药酶抑制剂。该发明意外地能够改善抗生素的活性。
• Hybrid molecules QA where Q is an aminoquinoline and A is an antibiotic residue, the synthesis and uses thereof as antibacterial agents
  申请人：Sanchez Muriel

  公开号：US20070060558A1

  公开（公告）日：2007-03-15

  The invention concerns an aminoquinoline-antibiotic hybrid compound of general formula (I): Q—(Y 1 ) p —(U) p —(Y 2 ) p -A: wherein Q represents an aminoquinoline, (Y 1 ) p (U) p —(Y 2 ) p″ is an optional spacer and A is an antibiotic residue. The invention enables the antibiotic residue activity to be unexpectedly enhanced.

  本发明涉及一种氨基喹啉-抗生素杂合物，其一般式为(I)：Q—(Y1)p—(U)p—(Y2)p-A，其中Q代表氨基喹啉，(Y1)p(U)p—(Y2)p″是可选的间隔基，A为抗生素残基。本发明使得抗生素残基的活性得到了意外的增强。
• Novel antimicrobial lactam-quinolones
  申请人：Norwich Eaton Pharmaceuticals, Inc.

  公开号：EP0366189A2

  公开（公告）日：1990-05-02

  Antimicrobial lactam-quinolone compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: wherein (1) A', A2, A3, R1, R4 and R6 generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have animicrobial activity; and (2) R' or R3 contain a linking moiety, linking the quinolone moiety to a lactam-containing moiety having the formula: wherein (3) R10, R11, R12, R13, and R14, together with bonds "a" and "b", form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and (4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, phosphone, phosphoramide, phosphate, sulfonamide, ester, thioester, amide, and hydrazide groups.

  抗菌内酰胺-喹诺酮化合物，包括与喹诺酮分子相连的含内酰胺分子，其分子式为 其中 (1) A'、A2、A3、R1、R4 和 R6 通常构成本领域已知的具有抗菌活性的各种喹诺酮、萘啶或相关环状分子中的任一种；以及 (2) R' 或 R3 含有连接基团，将喹诺酮基团与具有以下式子的含内酰胺基团连接起来： 其中 (3) R10、R11、R12、R13 和 R14 与键 "a "和 "b "一起构成本领域已知的具有抗菌活性的各种含内酰胺分子中的任一种；以及 (4) 连接分子包括（例如）氨基甲酸酯、二硫代氨基甲酸酯、脲、硫脲、异乌拉 铵、异硫乌拉铵、胍、碳酸盐、三硫代碳酸盐、反向氨基甲酸酯、黄原酸盐、反向异乌拉 铵、反向二硫代氨基甲酸酯、反向二硫代氨基甲酸酯、反向二硫代氨基甲酸酯、反向二硫代氨基甲酸酯、反向二硫代氨基甲酸酯、反向二硫代氨基甲酸酯、反向二硫代氨基甲酸酯、反转二硫代氨基甲酸酯、反转异硫脲、胺、亚胺、铵、杂芳脲、醚、硫醚、膦、磷酰胺、磷酸盐、磺酰胺、酯、硫酯、酰胺和酰肼基团。
• Methods for treating bacterial infection
  申请人：Innocoll Technologies Limited

  公开号：EP2510929A1

  公开（公告）日：2012-10-17

  This invention relates to methods for treating bacterial infection, which methods find utility in the treatment of, for example, infected ulcers, optionally infected diabetic ulcers. In particular, this invention relates to treating bacterial infection, for example, infected diabetic ulcers by topical administration of at least one aminoglycoside antibiotic at the site of infection, in combination with at least one antibacterial agent, which antibacterial agent is administered remote from the site of infection, preferably administered systemically. In a particular embodiment, the present invention relates to a composition for use in treating bacterial infection, the composition comprising gentamicin sulphate (a water-soluble broad-spectrum aminoglycoside antibiotic) uniformly dispersed in a type-I collagen matrix; in combination with at least one systemically-administered antibacterial agent. The present invention provides bactericidal activity against most strains of aerobic gram-negative and gram-positive and facultative anaerobic gram-negative pathogens, including methicillin-resistant Staphylococcus aureus.

  本发明涉及治疗细菌感染的方法，这些方法可用于治疗例如感染性溃疡，也可用于治疗感染性糖尿病溃疡。特别是，本发明涉及通过在感染部位局部施用至少一种氨基糖苷类抗生素，结合至少一种抗菌剂，治疗细菌感染，例如感染性糖尿病溃疡，该抗菌剂远离感染部位施用，最好是全身施用。在一个特定的实施方案中，本发明涉及一种用于治疗细菌感染的组合物，该组合物包括均匀分散在 I 型胶原基质中的硫酸庆大霉素（一种水溶性广谱氨基糖苷类抗生素）；与至少一种全身给药的抗菌剂结合使用。本发明对大多数需氧革兰阴性、革兰阳性和兼性厌氧革兰阴性病原体菌株具有杀菌活性，包括耐甲氧西林金黄色葡萄球菌。
• ISOLATION OF CLAVULANIC ACID FROM FERMENTATION BROTH BY ULTRAFILTRATION
  申请人：Lek Pharmaceutical and Chemical Co. D.D.

  公开号：EP0859780A1

  公开（公告）日：1998-08-26