H-Pro-MNA | 94720-65-7

• 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: H-Pro-MNA
• 英文别名: l-Proline-4-methoxy-2-naphthylamide；(2S)-N-(4-methoxynaphthalen-2-yl)pyrrolidine-2-carboxamide
• CAS: 94720-65-7
• 化学式: C₁₆H₁₈N₂O₂
• 分子量: 270.331
• InChiKey: MOERTZHMSVIRNL-AWEZNQCLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  50.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  H-Pro-MNA 、 pyridin-3-ylmethoxycarbonyl-Pro-Ala-Gly-OH 在 1-羟基苯并三唑 、 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 12.0h， 生成 Pyridin-3-ylmethoxycarbonyl-Pro-Ala-Gly-Pro-MNA
  参考文献：
  名称：

  FAP-activated anti-tumor compounds

  摘要：

  该发明涉及一种前药，它能够通过人类成纤维细胞活化蛋白（FAPα）的催化作用转化为药物，所述前药在生理条件下化学稳定，并可用于制备物理稳定的水性配方。它具有一个被FAPα识别的裂解位点，由FAPα的酶活性释放的药物在生理条件下具有细胞毒性或细胞静止作用。

  公开号：

  US20030232742A1

文献信息

• Microorganisms detection methods and the separation of agglutinated microorganisms, and a kit for use therein
  申请人：E-Y LABORATORIES, INC.

  公开号：EP0122023A1

  公开（公告）日：1984-10-17

  A test for the differential detection of suspected N. gonorrhoeae (N.g.) and N. meningitidis (N.m.) in provided by contacting a suspected sample with a lectin, preferably wheat germ agglutinin and either soy bean agglutinin or STA potato lectin. An agglutinin reaction is a positive indication of the presence of such microorganisms. Separate portions of the specimen may be contaced with fast substrates specific for (a) N.g., (b) N.m., and (c) B. catarrhalis. Suitable fast substrates are proline naphthylamide, gamma glutamyl naphthylamide, and glycyl prolyl naphthylamide, respectively, each substituted with an electron donating group at the 4-position, 6-position, or both. Another portion of the specimen may be reacted with a substrate for beta-galactosidase enzyme, a positive reaction being an indication that the specimen contains N.lactimica. Autoagglutination, which could otherwise give a false positive in the lectin test, may be prevented by pretreatment of the specimen with DNA'ase and/or an anhydride such as succinic anhydride.

  一种用于鉴别检测疑似淋球菌（N.g.）和脑膜炎双球菌（N.m.）的检测方法是将疑似样本与凝集素（最好是小麦胚芽凝集素和大豆凝集素或 STA 马铃薯凝集素）接触。凝集素反应是此类微生物存在的阳性指标。标本的不同部分可分别与(a) N.g.、(b) N.m.和(c) B. catarrhalis 的特异性快速底物反应。合适的快速底物分别是脯氨酸萘甲酰胺、γ-谷氨酰萘甲酰胺和甘氨酰脯氨酰萘甲酰胺，每种底物都在 4 位、6 位或两者上被电子捐赠基团取代。标本的另一部分可与β-半乳糖苷酶的底物反应，阳性反应表明标本中含有乳酸奈米卡氏菌。用 DNA'ase 和/或酸酐（如琥珀酸酐）对标本进行预处理，可防止自身凝集，否则会在凝集素检测中出现假阳性。
• Enzyme activities and pH tests for the determination of the risk of obstetric and gynecologic complications in samples of body fluids of women
  申请人：UNIBIO S.R.L.

  公开号：EP1528396A1

  公开（公告）日：2005-05-04

  The current invention describes a method for selecting a particular population of women having a risk of developing obstetric or gynecologic pathologies indicated as odds ratio (OR) value higher than 5.5, comprising the following steps in order: a) determination of the levels of sialidase by means of the procedure described in Cauci et al. Am J Obstet Gynecol 1998; 178; 511-5 and/or prolidase activity by means of the procedure described in Cauci et al. J Infect Dis 1998; 178; 1698-706 in samples of body fluid; b) determination of the pH value of said body fluid samples; c) selecting the samples having a sialidase value equal or above 5.0 nmol of methoxyphenol and/or a prolidase level equal or above 1500 mOD for prolidase and a pH ≥ 5.0. Consequently, this method gives the physician an efficient tool to decide whether or not to administer a pharmacological therapy to women at risk of severe adverse outcomes.

  本发明描述了一种选择特定妇女群体的方法，这些妇女患产科或妇科疾病的风险表示为几率比（OR）值高于5.5，该方法依次包括以下步骤： a) 通过 Cauci 等人，Am J Obstet Gynecol 1998; 178; 511-5 和/或 Cauci 等人，J Infect Dis 1998; 178; 1698-706 中描述的程序，测定体液样本中的葡萄糖苷酶水平； b) 确定所述体液样本的 pH 值； c) 挑选出硅糖苷酶值等于或高于 5.0 毫摩尔甲氧基苯酚和/或脯氨酸酶水平等于或高于 1500 毫摩尔脯氨酸酶且 pH 值≥5.0 的样本。 因此，这种方法为医生提供了一个有效的工具，以决定是否对有可能出现严重不良后果的妇女进行药物治疗。
• Enzymatic test for the determination of the risk of pathologies related to the presence of sialidase or prolidase activity in women body fluid samples
  申请人：——

  公开号：US20040219617A1

  公开（公告）日：2004-11-04

  The current invention describes a method for the determination of the risk of pathologies related to the presence of sialidase and/or prolidase activity in body fluid samples of women, comprising the following steps in order: a) determination of the levels of sialidase and/or prolidase activity in said sample of body fluid; b) comparison of said levels of sialidase and/or prolidase activity with ranges of prefixed values of said activity; c) calculation of the risk factor. This method resulted particularly efficient in permitting to obtain an accurate and reliable evaluation of the risk of pathologies related to the presence of sialidase and/or prolidase activity in samples of body fluid of women. Consequently, this method gives the physician an efficient tool to decide whether or not to administer a pharmacological therapy.

  本发明描述了一种测定与妇女体液样本中存在的葡萄糖苷酶和/或葡萄糖苷酶活性有关的病变风险的方法，该方法依次包括以下步骤： a) 确定所述体液样本中葡萄糖苷酶和/或脯氨酸酶活性的水平； b) 将所述硅氨酸酶和/或脯氨酸酶活性水平与所述活性的预设值范围进行比较； c) 计算风险系数。 这种方法特别有效，可以准确、可靠地评估与妇女体液样本中存在的葡萄糖苷酶和/或葡萄 糖苷酶活性有关的病变风险。因此，这种方法为医生提供了一种有效的工具，以决定是否进行药物治疗。
• ENZYMATIC TEST FOR THE DETERMINATION OF THE RISK OF PATHOLOGIES RELATED TO THE PRESENCE OF SIALIDASE OR PROLIDASE ACTIVITY IN WOMEN BODY FLUID SAMPLES
  申请人：UNIBIO S.R.L.

  公开号：EP1360484A1

  公开（公告）日：2003-11-12
• US5089394A
  申请人：——

  公开号：US5089394A

  公开（公告）日：1992-02-18