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(+/-)-2-(3-acetylamino-phenyl)-propionic acid amide | 117874-94-9

中文名称
——
中文别名
——
英文名称
(+/-)-2-(3-acetylamino-phenyl)-propionic acid amide
英文别名
(+/-)-2-(3-Acetylamino-phenyl)-propionsaeure-amid;2-(3-acetylamino)phenyl propionamide;2-(3-Acetamidophenyl)propanamide
(+/-)-2-(3-acetylamino-phenyl)-propionic acid amide化学式
CAS
117874-94-9
化学式
C11H14N2O2
mdl
——
分子量
206.244
InChiKey
QXSRXBXVLYFFIR-UHFFFAOYSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

计算性质

  • 辛醇/水分配系数(LogP):
    0.7
  • 重原子数:
    15
  • 可旋转键数:
    3
  • 环数:
    1.0
  • sp3杂化的碳原子比例:
    0.27
  • 拓扑面积:
    72.2
  • 氢给体数:
    2
  • 氢受体数:
    2

上下游信息

  • 上游原料
    中文名称 英文名称 CAS号 化学式 分子量

反应信息

  • 作为产物:
    描述:
    (+/-)-2-(3-acetylamino-phenyl)-propionic acid methyl ester 在 四氢呋喃ammonium hydroxide 作用下, 生成 (+/-)-2-(3-acetylamino-phenyl)-propionic acid amide
    参考文献:
    名称:
    99mTc-sestamibi muscle scintigraphy to assess the response to neuromuscular electrical stimulation of normal quadriceps femoris muscle
    摘要:
    Objectives: Neuromuscular electrical stimulation (NMES) is widely used for improving muscle strength by simultaneous contraction in the prevention of muscle atrophy. Although there exist many clinical methods for evaluating the therapeutic response of muscles, Tc-99m-sestamibi which is a skeletal muscle perfusion and metabolism agent has not previously been used for this purpose. The aim of our work was to ascertain whether Tc-99m-sestamibi muscle scintigraphy is useful in the monitoring of therapeutic response to NMES in healthy women.Methods: The study included 16 women aged between 21 and 45, with a mean age of 32.7 +/- 6.4. Both quadriceps femoris muscles (QFM) of each patient were studied. After randomization to remove the effect of the dominant side, one QFM of each patient was subjected to the NMES procedure for a period of 20 days. NMES was performed with an alternating biphasic rectangular current, from a computed electrical stimulator daily for 23 minutes. After measurement of skinfold thickness over the thigh, pre- and post-NMES girth measurements were assessed in centimeters. Sixty minutes after injections of 555 MBq Tc-99m-sestamibi, static images of the thigh were obtained for 5 minutes. The thigh-to-knee uptake ratio was calculated by semiquantitative analysis and normalized to body surface area (NUR = normalized uptake ratio).Results: The difference between the pre and post NMES NUR values was Significant (1.76 +/- 0.31 versus 2.25 +/- 0.38, p = 0.0000). The percentage (%) increase in NUR values also well correlated with the % increase in thigh girth measurements (r = 0.89, p = 0.0000).Conclusion: These results indicated that Tc-99m-sestamibi muscle scintigraphy as a new tool may be useful in evaluating therapeutic response to NMES.
    DOI:
    10.1007/bf02988252
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文献信息

  • 2-Arylpropionic Acid Derivatives and Pharmaceutical Compositions Containing Them
    申请人:Allegretti Marcello
    公开号:US20080312293A1
    公开(公告)日:2008-12-18
    The present invention relates to selected (R)-2-phenyl-propionamides and (R)-2-phenyl-sulfonamides with a hydrogen bond acceptor atom/group in a well defined position in the chemical space. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    本发明涉及在化学空间中具有氢键受体原子/基团的选定(R)-2-苯基-丙酰胺和(R)-2-苯基-磺酰胺。这些化合物表现出惊人的强烈抑制C5a诱导的人类PMN趋化性的效果。本发明的化合物绝对缺乏CXCL8抑制活性。所述化合物在治疗与补体C5a诱导的中性粒细胞和单核细胞趋化活化有关的病理过程中有用。特别是,在治疗败血症、牛皮癣、类风湿性关节炎、溃疡性结肠炎、急性呼吸窘迫综合征、特发性纤维化、肾小球肾炎以及缺血再灌注损伤的预防和治疗方面,本发明的化合物非常有用。
  • WO2006/63999
    申请人:——
    公开号:——
    公开(公告)日:——
  • 2-ARYLPROPIONIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    申请人:DOMPE' pha.r.ma S.p.A.
    公开号:EP1856031A1
    公开(公告)日:2007-11-21
  • US7939521B2
    申请人:——
    公开号:US7939521B2
    公开(公告)日:2011-05-10
  • [EN] 2-ARYLPROPIONIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] DÉRIVÉS DE L'ACIDE 2-ARYLPROPIONIQUE ET COMPOSITIONS PHARMACEUTIQUES CONTENANT CEUX-CI
    申请人:DOMPE SPA
    公开号:WO2006063999A1
    公开(公告)日:2006-06-22
    [EN] The present invention relates to selected (R)-2-phenyl-propionamides and (R)-2-phenyl-sulfonamides with a hydrogen bond acceptor atom/group in a well defined position in the chemical space. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    [FR] La présente invention concerne des (R)-2-phénylpropionamides et des (R)-2-phénylsulfonamides ayant un atome/groupe accepteur de liaison hydrogène en une position bien définie dans l'espace chimique. Ces composés présentent un effet inhibiteur puissant étonnant sur la chimiotaxie des PMN humains induite par le C5a. Les composés de l'invention n'ont absolument aucune activité d'inhibition de la CXCL8. Lesdits composés sont utiles dans le traitement de pathologies dépendantes de l'activation chimiotactique de neutrophiles et de monocytes induite par la fraction C5a du complément. En particulier, les composés de l'invention sont utiles dans le traitement de la sepsie, du psoriasis, de la polyarthrite rhumatoïde, de la recto-colite hémorragique, du syndrome de détresse respiratoire aiguë, de la fibrose idiopathique, de la glomérulonéphrite et dans la prévention et le traitement d'une plaie provoquée par l'ischémie et la reperfusion.
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