1-(2-Carboxyphenyl)-semicarbazid | 98488-38-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-(2-Carboxyphenyl)-semicarbazid
• 英文别名: 2-semicarbazido-benzoic acid；2-Semicarbazido-benzoesaeure；2-(2-Carbamoylhydrazinyl)benzoic acid
• CAS: 98488-38-1
• 化学式: C₈H₉N₃O₃
• 分子量: 195.178
• InChiKey: FOXJFGIZEDWSCJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  104
• 氢给体数：
  4
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(2-Carboxyphenyl)-semicarbazid 、 alkaline earth salt of/the/ methylsulfuric acid 、 alkaline earth salt of/the/ methylsulfuric acid 生成 (2-Carboxy-benzolazo)-ameisensaeure-amid
  参考文献：
  名称：

  Potential novel predictors of mortality in end-stage renal disease patients with sleep disorders

  摘要：

  Patients with end-stage renal disease (ESRD) have an annual mortality rate exceeding 20%, although some survive many years. The ESRD population has a high incidence of sleep disorders, including sleep apnea and periodic limb movements in sleep (PLMS), Sleep disorders result in sleep deprivation, which can negatively affect immune function and cardiovascular-related outcomes, common causes of death in patients with ESRD. This study examined predictors of mortality in patients with ESRD with sleep problems. Twenty-nine consecutive patients with ESRD reporting disrupted sleep or daytime sleepiness were studied by all-night polysomnography. All patients were followed up until death, transplantation, or study termination, Among the variables studied, including such previously reported predictors as serum albumin level, urea reduction ratio, and hematocrit, only the PLMS index (PLMSI), arousing PLMSI (APLMSI), and total number of arousals per hour of sleep significantly predicted mortality, The 20-month survival rate with a PLMSI less than 20 was greater than 90% versus 50% for a PLMSI of 20 or greater (exact log-rank, P = 0.007), For the deceased versus survivor groups, mean PLMSI was 119.1 versus 19.8 (P = 0.01) and APLMSI was 48.1 versus 7.8 (P = 0.00006), with a mean survival of 10.3 versus greater than 25.5 months, respectively (P = 0.001), Median survival of patients with a PLMSI greater than 80 was only 6 months, PLMSI, APLMSI, and total arousals per hour of sleep were strongly associated with mortality in patients with ESRD with sleep disorders independent of other factors and may be novel predictors of near-term mortality. (C) 2000 by the National Kidney Foundation, Inc.

  DOI：

  10.1016/s0272-6386(00)70039-4
• 作为产物：
  描述：

  potassium cyanate 、 alkaline earth salt of/the/ methylsulfuric acid 在 氢氧化钾 作用下， 生成 1-(2-Carboxyphenyl)-semicarbazid
  参考文献：
  名称：

  Potential novel predictors of mortality in end-stage renal disease patients with sleep disorders

  摘要：

  Patients with end-stage renal disease (ESRD) have an annual mortality rate exceeding 20%, although some survive many years. The ESRD population has a high incidence of sleep disorders, including sleep apnea and periodic limb movements in sleep (PLMS), Sleep disorders result in sleep deprivation, which can negatively affect immune function and cardiovascular-related outcomes, common causes of death in patients with ESRD. This study examined predictors of mortality in patients with ESRD with sleep problems. Twenty-nine consecutive patients with ESRD reporting disrupted sleep or daytime sleepiness were studied by all-night polysomnography. All patients were followed up until death, transplantation, or study termination, Among the variables studied, including such previously reported predictors as serum albumin level, urea reduction ratio, and hematocrit, only the PLMS index (PLMSI), arousing PLMSI (APLMSI), and total number of arousals per hour of sleep significantly predicted mortality, The 20-month survival rate with a PLMSI less than 20 was greater than 90% versus 50% for a PLMSI of 20 or greater (exact log-rank, P = 0.007), For the deceased versus survivor groups, mean PLMSI was 119.1 versus 19.8 (P = 0.01) and APLMSI was 48.1 versus 7.8 (P = 0.00006), with a mean survival of 10.3 versus greater than 25.5 months, respectively (P = 0.001), Median survival of patients with a PLMSI greater than 80 was only 6 months, PLMSI, APLMSI, and total arousals per hour of sleep were strongly associated with mortality in patients with ESRD with sleep disorders independent of other factors and may be novel predictors of near-term mortality. (C) 2000 by the National Kidney Foundation, Inc.

  DOI：

  10.1016/s0272-6386(00)70039-4

文献信息

• NOVEL SUBSTITUTED-1-H-QUINAZOLINE-2,4-DIONE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
  申请人：Seong Churlmin

  公开号：US20090203708A1

  公开（公告）日：2009-08-13

  Disclosed herein are novel substituted-1H-quinazoline-2,4-dione derivatives, a preparation method thereof, and a pharmaceutical composition containing the same. The novel substituted-1H-quinazoline-2,4-dione derivatives are excellent in binding affinity and selectivity for 5-HT6 receptors over other receptors, inhibit serotonin(5-HT)-stimulated cAMP accumulation, and disrupt apomorphine(2 mg/kg, i.p.)-induced hyperactivity in rats. Thanks to these effects, the derivatives are useful in the treatment of 5-HT6 receptor-related central nervous system diseases.

  本文披露了一种新型的取代-1H-喹唑啉-2,4-二酮衍生物，其制备方法以及含有该衍生物的药物组合物。这种新型的取代-1H-喹唑啉-2,4-二酮衍生物在与其他受体相比对5-HT6受体的结合亲和力和选择性方面表现出色，抑制5-羟色胺（5-HT）刺激的cAMP积累，并破坏大鼠中阿波莫啡（2 mg/kg，i.p.）诱导的过度活动。由于这些效果，这些衍生物在治疗与5-HT6受体相关的中枢神经系统疾病中非常有用。
• NOVEL SUBSTITUTED-1H-QUINAZOLINE-2,4-DIONE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
  申请人：KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

  公开号：EP2035406A1

  公开（公告）日：2009-03-18
• EP2035406A4
  申请人：——

  公开号：EP2035406A4

  公开（公告）日：2009-08-05
• [EN] NOVEL SUBSTITUTED-1H-QUINAZOLINE-2,4-DIONE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME<br/>[FR] NOUVEAUX DÉRIVÉS SUBSTITUÉS DE 1H-QUINAZOLINE-2,4-DIONE, PROCÉDÉ DE PRÉPARATION DE CES DERNIERS ET COMPOSITION PHARMACEUTIQUE CONTENANT LESDITS DÉRIVÉS
  申请人：KOREA RESERACH INST OF CHEMICA

  公开号：WO2008004716A1

  公开（公告）日：2008-01-10

  [EN] Disclosed herein are novel substituted-lH-quinazoline-2,4-dione derivatives, a preparation method thereof, and a pharmaceutical composition containing the same. The novel substituted- lH-quinazoline-2,4-dione derivatives are excellent in binding affinity and selectivity for 5-HT6 receptors over other receptors, inhibit serotonin(5-HT)-stimulated cAMP accumulation, and disrupt apomorphine(2 mg/kg, i.p.)-induced hyperactivity in rats. Thanks to these effects, the derivatives are useful in the treatment of 5-HT6 receptor-related central nervous system diseases.
  [FR] L'invention concerne de nouveaux dérivés substitués de 1H-quinazoline-2,4-dione, un procédé de préparation de ces derniers, ainsi qu'une composition pharmaceutique contenant lesdits dérivés. Les nouveaux dérivés de 1H-quinazoline-2,4-dione présentent une affinité de liaison et une sélectivité pour les récepteurs 5-HT6 excellentes comparé à d'autres récepteurs, inhibent l'accumulation d'AMPc stimulée par la sérotonine (5-HT), et mettent fin à l'hyperactivité induite par l'apomorphine (2 mg/kg, i-p.) chez les rats. Du fait desdits effets, lesdits dérivés sont utiles dans le traitement de maladies du système nerveux central liées aux récepteurs 5-HT6.