(2R,5R)-L-[艹孟]基-5-(乙酰氧基)-1,3-噁噻戊环-2-羧酸酯 | 125319-03-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: (2R,5R)-L-[艹孟]基-5-(乙酰氧基)-1,3-噁噻戊环-2-羧酸酯
• 中文别名: 3-羧基苯基苯基乙酰氨基甲基膦酸酯
• 英文名称: 3-Carboxyphenyl phenylacetamidomethylphosphonate
• 英文别名: 3-[hydroxy-[[(2-phenylacetyl)amino]methyl]phosphoryl]oxybenzoic acid
• CAS: 125319-03-1
• 化学式: C₁₆H₁₆NO₆P
• 分子量: 349.27
• InChiKey: PQNMYMXNEUQFAJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  24
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  113
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• PYRAZOLE COMPOUNDS HAVING THERAPEUTIC EFFECT ON MULTIPLE MYELOMA
  申请人：Nishino Taito

  公开号：US20130253204A1

  公开（公告）日：2013-09-26

  Novel therapeutic agents for myeloma are provided. A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R 1 is C 1 -C 6 alkyl, C 1 -C 6 alkyl substituted with R 17 , C 1 -C 6 haloalkyl, phenyl, phenyl substituted with a R 11 's or the like, R 2 is a hydrogen atom, C 1 -C 6 alkyl, phenyl or phenyl optionally substituted with e R 21 's or the like, R 3 is a hydrogen atom or the like, X is a single bond or —(CR 6 , R 7 ) n —, each of R 4 and R 5 is independently C 1 -C 6 alkyl or the like, R 6 and R 7 are hydrogen atoms or C 1 -C 6 alkyl, R 8 is phenyl, phenyl optionally substituted with k R 81 's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.

  提供了用于骨髓瘤的新型治疗药物。一种用于多发性骨髓瘤的治疗剂，包含由式（1）表示的吡唑烷化合物：其中R1是C1-C6烷基，C1-C6烷基取代为R17，C1-C6卤代烷基，苯基，苯基取代为R11或类似物，R2是氢原子，C1-C6烷基，苯基或可选地取代为e个R21或类似物，R3是氢原子或类似物，X是单键或—（CR6，R7)n—，R4和R5分别独立地是C1-C6烷基或类似物，R6和R7是氢原子或C1-C6烷基，R8是苯基，苯基可选地取代为k个R81或类似物，所述化合物的互变异构体或其药用上可接受的盐或溶剂，作为活性成分。
• Bismuth compounds for the treatment and prevention of mucositis
  申请人：GelTex Pharmaceuticals, Inc.

  公开号：US20020081340A1

  公开（公告）日：2002-06-27

  The invention relates to the unexpected discovery that bismuth-containing compounds are effective in the treatment of oral mucositis in a mammal. Thus, the invention relates, in one aspect to a method of treating oral mucositis comprising administering an effective amount of a pharmaceutically acceptable bismuth-containing compound, such as a bismuth salt or bismuth complex. In a preferred embodiment, the bismuth compound is an organic or inorganic salt such as, bismuth subsalicylate, bismuth subgallate, bismuth aluminate, bismuth citrate, bismuth subcitrate, bismuth carbonate, bismuth subcarbonate, tripotassium dicitrato bismuthate, bismuth nitrate, bismuth subnitrate, bismuth tartrate and mixtures thereof, preferably, bismuth subsalicylate and bismuth subgallate.

  本发明涉及到一种意外发现：含铋化合物在哺乳动物的口腔粘膜炎症治疗中具有有效性。因此，本发明在一个方面涉及到一种治疗口腔粘膜炎症的方法，包括给予有效量的药用可接受的含铋化合物，例如铋盐或铋配合物。在一个优选实施例中，铋化合物是有机或无机盐，例如铋亚水杨酸盐、铋亚没食子酸盐、铋铝酸盐、铋柠檬酸盐、铋亚柠檬酸盐、铋碳酸盐、铋亚碳酸盐、三钾柠檬酸铋酸盐、铋硝酸盐、铋亚硝酸盐、铋酒石酸盐及其混合物，优选地，铋亚水杨酸盐和铋亚没食子酸盐。
• Identification of sortase gene
  申请人：——

  公开号：US20030022178A1

  公开（公告）日：2003-01-30

  The present invention is a substantially purified sortase-transamidase enzyme from Gram-positive bacteria, such as Staphylococcus aureus . The enzyme having a molecular weight of about 23,539 or about 29,076 daltons and catalyzing a reaction that covalently cross-links the carboxyl terminus of a protein having a sorting signal to the peptidoglycan of a Gram-positive bacterium, the sorting signal having: (1) a motif of LPX 3 X 4 G therein; (2) a substantially hydrophobic domain of at least 31 amino acids carboxyl to the motif; and (3) a charged tail region with at least two positively charged residues carboxyl to the substantially hydrophobic domain, at least one of the two positively charged residues being arginine, the two positively charged residues being located at residues 31-33 from the motif, wherein X 3 is any of the twenty naturally-occurring L-amino acids and X 4 is selected from the group consisting of alanine, serine, and threonine, and wherein sorting occurs by cleavage between the fourth and fifth residues of the LPX 3 X 4 G motif. Variants of the enzyme, methods for cloning the gene encoding the enzyme and expressing the cloned gene, and methods of use of the enzyme, including for screening for antibiotics and for display of proteins or peptides on the surfaces of Gram-positive bacteria, are also disclosed.

  本发明是一种从革兰氏阳性细菌（如 金黄色葡萄球菌 .该酶的分子量约为 23,539 或 29,076 道尔顿，可催化将具有分选信号的蛋白质的羧基端与革兰氏阳性细菌的肽聚糖共价交联的反应，分选信号具有：(1) LPX 3 X 4 G的基序；(2) 与基序羧基化的至少有 31 个氨基酸的基本疏水结构域；(3) 与基本疏水结构域羧基化的至少有两个带正电的残基的带电尾区，这两个带正电的残基中至少有一个是精氨酸，这两个带正电的残基位于基序的残基 31-33 处，其中 X 3 是二十种天然存在的 L-氨基酸中的任何一种，X 4 选自丙氨酸、丝氨酸和苏氨酸组成的组，其中分选通过 LPX 的第四和第五个残基之间的裂解进行 3 X 4 G motif。此外，还公开了该酶的变体、克隆编码该酶的基因和表达克隆基因的方法，以及该酶的使用方法，包括用于筛选抗生素和在革兰氏阳性细菌表面显示蛋白质或肽的方法。
• Method for treating alcoholic hepatitis
  申请人：Fink P. Mitchell

  公开号：US20050032891A1

  公开（公告）日：2005-02-10

  Disclosed is a method for treating acute alcoholic hepatitis in a subject. The method comprises the step of administering to the subject an effective amount of an ester of an alpha-ketoalkanoic acid or an amide of an alpha-ketoalkanoic acid.

  本发明公开了一种治疗受试者急性酒精性肝炎的方法。该方法包括向受试者施用有效量的α-酮烷酸的酯或α-酮烷酸的酰胺。
• Methods and compositions involving sortase B
  申请人：Schneewind Olaf

  公开号：US20060073530A1

  公开（公告）日：2006-04-06

  The present invention provides methods and compositions involving sortase-transamidases, including sortase B, and polypeptides that include a signal sorting sequence of NPQ/KTN/G. Methods of screening for inhibitors of Gram-positive bacteria as well as therapeutic, preventative, and research methods focusing on Gram-positive bacteria are also provided.

  本发明提供了涉及分选酶-转酰胺酶（包括分选酶 B）和包括 NPQ/KTN/G 信号分选序列的多肽的方法和组合物。本发明还提供了筛选革兰氏阳性细菌抑制剂的方法以及针对革兰氏阳性细菌的治疗、预防和研究方法。