N-formylmethionylphenylalanine | 22008-60-2

• 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: N-formylmethionylphenylalanine
• 英文别名: N-(N-Formyl-L-methionyl)-L-phenylalanine；(2S)-2-[[(2S)-2-formamido-4-methylsulfanylbutanoyl]amino]-3-phenylpropanoic acid
• CAS: 22008-60-2
• 化学式: C₁₅H₂₀N₂O₄S
• mdl: MFCD00056169
• 分子量: 324.401
• InChiKey: VZQJQFGSAAGNSI-STQMWFEESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  22
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  121
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N-formylmethionylphenylalanine 、 (N-β-aminoethylamino)colchicine 在 N,N'-二环己基碳二亚胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 20.0h， 生成
  参考文献：
  名称：

  C-10 amino acid derivatives of colchicine

  摘要：

  DOI：

  10.1007/bf00630252

文献信息

• Pharmaceutical administration systems containing chemotactic peptides
  申请人：THE BOARD OF REGENTS THE UNIVERSITY OF TEXAS SYSTEM

  公开号：EP0256989A1

  公开（公告）日：1988-02-24

  The present invention relates to pharmaceutical administration systems containing phophatidylserine and phosphatidylcholine or phosphatidylethanolamine derivatives in the form of liposomes which encapsulate chemotactic peptides such as N-formyl-L-methionyl-L-leucyl-L-phenylalanine. The liposomes are prepared by conventional dispersion methods. The pharmaceutical administration systems when applied in the form of liposomes stimulate macrophage activity which is especially useful in the cancer therapy for combating metastatic tumor cells and for treatment of chronic infections.

  本发明涉及含有磷脂酰丝氨酸和磷脂酰胆碱或磷脂酰乙醇胺衍生物的脂质体形式的给药系统，该脂质体包封了趋化肽，如 N-甲酰基-L-蛋氨酰-L-亮氨酰-L-苯丙氨酸。脂质体采用传统的分散方法制备。以脂质体形式使用的药物给药系统可刺激巨噬细胞的活性，尤其适用于癌症治疗，以对抗转移性肿瘤细胞和治疗慢性感染。
• A new antimicrobial compound,WF11605,derivatives therof and processes for preparing the same
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0330334A1

  公开（公告）日：1989-08-30

  Compounds of the formula: wherein R¹ is hydrogen or acyl, R² is hydrogen or in which R⁴, R⁵, R⁶ and R⁷ are hydrogen or acyl, R³ is carboxy or protected carboxy, and pharmaceutically acceptable salts thereof. One of these compounds, designated WF11605, can be prepared by culturing a WF11605 - producing microorganism, such as Agonomycetes strain F-11605, in an aqueous nutrient medium under aerobic conditions. Processes are also provided for the preparation of various synthetic derivatives of WF11605. The compound WF11605 and its derivatives possess antimicrobial activity and are useful as antibiotics and as agents for the prevention and treatment of diseases caused by Leukotriene B₄ (LTB₄). Pharmaceutical compositions containing these compounds are described.

  式中的化合物： 其中 R¹ 是氢或酰基、 R² 是氢或 其中 R⁴、R⁵、R⁶ 和 R⁷ 是氢或酰基、 R³ 是羧基或受保护的羧基、 及其药学上可接受的盐类。 这些化合物中的一种，命名为 WF11605，可以通过在有氧条件下在水性营养培养基中培养产生 WF11605 的微生物，如 Agonomycetes 菌株 F-11605 来制备。此外，还提供了制备 WF11605 的各种合成衍生物的工艺。 化合物 WF11605 及其衍生物具有抗菌活性，可用作抗生素以及预防和治疗由白三烯 B₄（LTB₄）引起的疾病的药物。本文介绍了含有这些化合物的药物组合物。
• Methods and compositions for reducing neurodegeneration in amyotrophic lateral sclerosis
  申请人：Yoo, Seo Hong

  公开号：EP2255812A1

  公开（公告）日：2010-12-01

  A composition comprising a clear aqueous solution comprising: (a) a first material selected from soluble ursodeoxycholic acid or a sodium salt oftauroursodeoxycholic acid (TUDCA); (b) a carbohydrate selected from the group consisting of an aqueous soluble starch conversion product or an aqueous soluble non-starch polysaccharide; (c) water, wherein the first material and the carbohydrate both remain in solution for any subset of the range of pH values obtainable in an aqueous system sufficient for a pharmaceutical formulation to remain in solution from preparation, to administration, to absorption in the body; for use in the treatment of at least one symptom of a neurodegenerative disease or at least one symptom of a motor neuron disease in a subject.

  一种由透明水溶液组成的组合物，其中包括 (a) 第一种材料，选自可溶性熊去氧胆酸或熊去氧胆酸钠盐 (TUDCA)； (b) 选自水溶性淀粉转化产物或水溶性非淀粉多糖的碳水化合物； (c) 水，其中第一种材料和碳水化合物在水体系中可获得的 pH 值范围的任何子集中均 保持溶液状态，足以使药物制剂从制备、给药到在体内吸收均保持溶液状态； 用于治疗受试者神经退行性疾病的至少一种症状或运动神经元疾病的至少一种症状。
• Functional inactivation of cxcr4-mediated responses in growth hormone transgenic mice through socs53 upregulation
  申请人：Martinez-Alonzo Carlos

  公开号：US20050221287A1

  公开（公告）日：2005-10-06

  A method is provided of identifying compounds for use in a pharmaceutical composition having an anti-viral effect against CXCR4-dependent HIV activity comprising: providing a first aliquot of CXCR-4-expressing GH-Tg cells; contacting said first aliquot with HIV particles; providing a second aliquot of CXCR4-expressing GH-Tg cells; contacting said second aliquot with a test ligand; contacting said second aliquot with HIV particles; and isolating virus from said first and said second aliquot of cells, wherein a decrease in the ability to isolate virus from said second aliquot cells indicates said test ligand possess anti-viral activity against HIV. Also provided is a method of identifying compounds for use in a pharmaceutical composition having a therapeutic effect against a disease involving CXCR4-dependent chemotaxis comprising providing a first aliquot CXCR4-expressing GH-Tg cells; contacting said first aliquot with CXCL12; measuring a first migration indes; providing a second aliquot of CXCR4-expressing GH-Tg cells; contacting said second aliquot with CXCL12; contacting said second aliquot with a test ligand; measuring a second migration index; and determing a therapeutic potential. In addition, compounds for us in a pharmaceutical composition having a therapeutic effect against a SOCS3 inhibitable disease are identified by a method comprising: providing a first cell having at least one chemokine receptor expressed thereon, said first cell having been transfected with at least one SOCS construct; contacting said first cell with at least one chemokine, measuring a first migration index; providing a second cell having at least one chemokine receptor expressed thereon, said second cell having been transfected with at least one SOCS construct; contacting said second cell with at least one chemokine; measuring a second migration index; and determining a therapeutic potential subjects having a disease associated with CXCR4-dependent HIV are treated by administering to said subject a therapeutically anti-viral effective amount of a compound that induces the expression of SOCS3 and a pharmaceutically acceptable carrier.

  本发明提供了一种鉴定化合物的方法，该化合物可用于具有抗病毒作用的药物组合物中，该药物组合物具有抗CXCR4依赖性HIV活性，该方法包括提供表达CXCR-4的GH-Tg细胞的第一等分试样；将所述第一等分试样与HIV颗粒接触；提供表达CXCR4的GH-Tg细胞的第二等分试样；将所述第二等分试样与测试配体接触；将所述第二等分试样与HIV颗粒接触；以及从所述第一和所述第二等分试样细胞中分离病毒，其中从所述第二等分试样细胞中分离病毒的能力下降表明所述测试配体具有抗HIV的抗病毒活性。本发明还提供了一种用于鉴定对涉及 CXCR4 依赖性趋化的疾病具有治疗作用的药物组合物中的化合物的方法，该方法包括提供第一等分的表达 CXCR4 的 GH-Tg 细胞；使所述第一等分细胞与 CXCL12 接触；测量第一迁移指数；提供第二等分的表达 CXCR4 的 GH-Tg 细胞；使所述第二等分细胞与 CXCL12 接触；使所述第二等分细胞与测试配体接触；测量第二迁移指数；以及确定治疗潜力。此外，还通过以下方法鉴定了药物组合物中对 SOCS3 可抑制疾病具有治疗效果的化合物：提供具有至少一种趋化因子受体的第一细胞，所述第一细胞已转染至少一种 SOCS 构建物；使所述第一细胞与至少一种趋化因子接触，测量第一迁移指数；提供具有至少一种趋化因子受体的第二细胞，所述第二细胞已转染至少一种 SOCS 构建物；将所述第二细胞与至少一种趋化因子接触；测量第二迁移指数；以及确定治疗潜力 通过向所述受试者施用治疗抗病毒有效量的诱导 SOCS3 表达的化合物和药学上可接受的载体，治疗患有与 CXCR4 依赖性 HIV 相关疾病的受试者。
• METHOD OF DETECTING ADHERENT CELLS
  申请人：MINNESOTA MINING AND MANUFACTURING COMPANY

  公开号：EP0026214A1

  公开（公告）日：1981-04-08