2-[(benzyloxy-formyl-amino)-methyl]-hexanoic acid | 773867-93-9

• 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-[(benzyloxy-formyl-amino)-methyl]-hexanoic acid
• 英文别名: 2R-[(benzyloxy-formylamino)-methyl]-hexanoic acid；2-(Phenylmethoxycarbonylaminomethyl)hexanoic acid
• CAS: 773867-93-9
• 化学式: C₁₅H₂₁NO₄
• 分子量: 279.336
• InChiKey: OQFXWRRVLVYKMU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  20
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  75.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(吡啶-2)-吡咯烷 、 2-[(benzyloxy-formyl-amino)-methyl]-hexanoic acid 生成 N-hydroxy-N-[3(R)-(2-R/S-pyridin-2-yl-pyrrolidine-1-carbonyl)-hexyl]-formamide
  参考文献：
  名称：

  Novel pyrrolidine bicyclic compounds and its derivatives, compositions and methods of use

  摘要：

  N-[1-氧代-(可选2-氮代)-2-烷基-3-(羧基或硫醇或羟胺羰基或N-羟甲酰胺基)-丙基]-(芳基或杂环芳基)-氮代环4-7烷烃或硫氮代环4-7烷烃，其盐或前药具有有趣的性质，例如，在通过PDF抑制剂治疗或预防适于通过PDF抑制剂治疗的疾病，如治疗细菌感染方面。

  公开号：

  US20030069223A1

文献信息

• N-Formyl Hydrozyamine Compounds
  申请人：Lee Kwangho

  公开号：US20090062537A1

  公开（公告）日：2009-03-05

  Novel N-formyl hydroxylamine compounds and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed.

  本发明公开了新型N-甲酰基羟胺化合物及其衍生物。这些N-甲酰基羟胺化合物可以抑制肽脱甲酰酶（PDF），该酶存在于原核生物中。这些化合物作为抗菌素和抗生素具有用途。本发明的化合物对肽脱甲酰酶相对于其他金属蛋白酶如MMPs表现出了选择性抑制作用。还公开了这些化合物的制备方法和用途。
• Hydroxamic acid or n-formyl hydroxylamine derivatives as inhibitors of bakterial polypeptide deformylase for treating microbial infections
  申请人：——

  公开号：US20040106666A1

  公开（公告）日：2004-06-03

  1 Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(═O) or formula C(═O)NH(OH); R 1 represents hydrogen, methyl or trifluromethyl, or except when Z is a radical of formula —N(OH)(═O), a hydroxy, halo or am group; R 2 represents a group R 10 —(X) n -(ALK) m — wherein R 10 , ALK, X, m and n are as defined in the specification; R 3 represents hydrogen, (C 1 -C 6 ) alkyl or phenyl(C 1 -C 6 )alkyl-; and R 5 and R 6 are as defined in the specification.

  公式（I）的化合物是用于治疗人类和非人哺乳动物感染的抗菌或抗原虫药物，其中：Z代表公式—N（OH）CH（═O）或公式C(═O)NH(OH)的基团；R1代表氢、甲基或三氟甲基，或者除非Z是公式—N(OH)(═O)的基团，否则是一个羟基、卤素或氨基；R2代表一个基团R10—(X)n-(ALK)m—，其中R10、ALK、X、m和n如规范中所定义；R3代表氢、（C1-C6）烷基或苯基（C1-C6）烷基；R5和R6如规范中所定义。
• Novel N-formyl hydroxylamine compounds, compositions and methods of use
  申请人：——

  公开号：US20030045479A1

  公开（公告）日：2003-03-06

  N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl]-(carbonylamino-aryl or -heteroaryl)-azacyclo 4-7 alkanes or thiazacyclo 4-7 alkanes or imidazacyclo 4-7 alkanes have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections.

  N-[1-氧代-2-烷基-3-(N-羟基甲酰胺基)-丙基]-(羰基氨基-芳基或-杂环芳基)-氮杂环4-7烷烃或硫氮杂环4-7烷烃或咪唑氮杂环4-7烷烃具有有趣的特性，例如在治疗或预防适合使用肽变形酶抑制剂治疗的疾病，如细菌感染的治疗。
• Antimicrobial agents
  申请人：——

  公开号：US20040102491A1

  公开（公告）日：2004-05-27

  Compounds of formula (I) and (IA) have antibacterial or antiprotozoal activity: formula (1) formula (2) wherein: Z represents a radical of formula N(OH)CH(═O) or of formula C(═O)NH(OH); R 1 represents hydrogen, methyl or trifluoromethyl, or, except when Z is a radical of formula N(OH)CH(═O), a hydroxy or amino group; R 2 represents a radical of formula R 10 —(X) n -(ALK) m — wherein R 10 represents hydrogen, or an optionally substituted c 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, ALK represents a straight or branched divalent C 1 -C 6 alkylene, C 2 -C 6 ?alkenylene, or C 2 -C 6 alkynylene radical, and may be interrupted by one or more non-adjacent NH—, —O— or S— linkages, X represents NH—, —O— or S—, and m and n are independently 0 or 1; R 3 represents hydrogen, C 1 -C 6 alkyl, or benzyl; and R 4 is as defined in the specification.

  式(I)和(IA)的化合物具有抗菌或抗原虫活性：式(1)式(2)其中：Z代表式N(OH)CH(═O)或式C(═O)NH(OH)的基团；R1代表氢、甲基或三氟甲基，或者除非Z是式N(OH)CH(═O)的基团时，还可以是羟基或氨基；R2代表式R10—(X)n-(ALK)m—的基团，其中R10代表氢，或者是一个可选择地取代的C1-C6烷基、C2-C6烯基、C2-C6炔基、环烷基、芳基或杂环烷基，ALK代表直链或支链的二价C1-C6烷基、C2-C6烯基或C2-C6炔基基团，并且可能被一个或多个非相邻的NH—、—O—或S—连接所中断，X代表NH—、—O—或S—，m和n独立地为0或1；R3代表氢、C1-C6烷基或苄基；而R4如规范中所定义。
• [EN] ANTIMICROBIAL AGENTS<br/>[FR] AGENTS ANTIMICROBIENS
  申请人：BRITISH BIOTECH PHARM

  公开号：WO2000061134A1

  公开（公告）日：2000-10-19

  Compounds of formula (I) are antibacterial agents wherein: Z represents a radical of formula -N(OH)CH(=O) of formula -C(=O)NH(OH) and R1-R4 are as defined in the specification.

  公式（I）的化合物是抗菌剂，其中：Z代表公式-N（OH）CH（=O）的基团或公式-C（=O）NH（OH）的基团，而R1-R4如规范中所定义。