N-hydroxy 4-pyridineacetamide | 83421-27-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: N-hydroxy 4-pyridineacetamide
• 英文别名: N-hydroxy-2-pyridin-4-ylacetamide
• CAS: 83421-27-6
• 化学式: C₇H₈N₂O₂
• 分子量: 152.153
• InChiKey: RINWLNQPRDPPJT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  62.2
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-hydroxy 4-pyridineacetamide 、 7β-<2-(2-aminothiazol-4yl)-2-(Z)-methoximinoacetamide>-3-iodomethyl-2-<(trimethylsilyloxy)carbonyl>cephalosporin 在 甲醇 作用下， 生成 (6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-[[4-[2-(hydroxyamino)-2-oxoethyl]pyridin-1-ium-1-yl]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
  参考文献：
  名称：

  Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins

  摘要：

  The preparation and biological evaluation of a series of 7 beta-[2-(2-aminothiazol-4-yl)-2(Z)-methoximinoacetamido]cep halosporins, substituted at the 3'-position with monocyclic or bicyclic nitrogen-containing heterocycles are described. The resulting family of parenteral compounds displays a broad spectrum of antibacterial activity. Some compounds exhibit a similar level of Gram-negative activity to that of the "third-generation" cephalosporins with increased staphylococcal activity. The in vitro and in vivo antimicrobial activity, structure-activity relationships, beta-lactamase stability, and in vitro and in vivo pharmacological evaluations are presented.

  DOI：

  10.1021/jm00170a011
• 作为产物：
  描述：

  4-吡啶乙酸盐酸盐 在 盐酸羟胺 、 N,N'-羰基二咪唑 作用下， 以 水 、 N,N-二甲基甲酰胺 为溶剂， 生成 N-hydroxy 4-pyridineacetamide
  参考文献：
  名称：

  Cephalosporin antibiotics

  摘要：

  头孢菌素抗生素由以下公式代表##STR1##其中R为氢、C.sub.1-C.sub.4烷基或一个羧基取代的烷基基团；R.sub.1为H或C.sub.1-C.sub.4烷基；n为0、1或2；A和A'独立地为氢、C.sub.1-C.sub.4烷基或烯丙基；以及它们的药用盐是用于治疗哺乳动物的革兰氏阳性和革兰氏阴性感染的广谱抗生素。

  公开号：

  US04336253A1

文献信息

• BROWN, RAYMOND F.;KINNICK, MICHAEL D.;MORIN, JOHN M. (JR);VASILEFF, ROBER+, J. MED. CHEM., 33,(1990) N, C. 2114-2121
  作者：BROWN, RAYMOND F.、KINNICK, MICHAEL D.、MORIN, JOHN M. (JR)、VASILEFF, ROBER+

  DOI：——

  日期：——
• Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins
  作者：Raymond F. Brown、Michael D. Kinnick、John M. Morin、Robert T. Vasileff、Fred T. Counter、Edward O. Davidson、Paul W. Ensminger、Judith A. Eudaly、Jeffrey S. Kasher

  DOI：10.1021/jm00170a011

  日期：1990.8

  The preparation and biological evaluation of a series of 7 beta-[2-(2-aminothiazol-4-yl)-2(Z)-methoximinoacetamido]cep halosporins, substituted at the 3'-position with monocyclic or bicyclic nitrogen-containing heterocycles are described. The resulting family of parenteral compounds displays a broad spectrum of antibacterial activity. Some compounds exhibit a similar level of Gram-negative activity to that of the "third-generation" cephalosporins with increased staphylococcal activity. The in vitro and in vivo antimicrobial activity, structure-activity relationships, beta-lactamase stability, and in vitro and in vivo pharmacological evaluations are presented.
• Cephalosporin antibiotics
  申请人：Eli Lilly and Company

  公开号：US04336253A1

  公开（公告）日：1982-06-22

  Cephalosporin antibiotics represented by the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.4 alkyl or a carboxy substituted alkyl group; R.sub.1 is H or C.sub.1 -C.sub.4 alkyl; n is 0, 1 or 2; and A and A' independently are hydrogen, C.sub.1 -C.sub.4 alkyl or allyl; and pharmaceutically acceptable salts thereof are broad spectrum antibiotics useful in the treatment of gram positive and gram negative infections of mammals.

  头孢菌素抗生素由以下公式代表##STR1##其中R为氢、C.sub.1-C.sub.4烷基或一个羧基取代的烷基基团；R.sub.1为H或C.sub.1-C.sub.4烷基；n为0、1或2；A和A'独立地为氢、C.sub.1-C.sub.4烷基或烯丙基；以及它们的药用盐是用于治疗哺乳动物的革兰氏阳性和革兰氏阴性感染的广谱抗生素。