5-methyl-1(2)H-pyrazole-3-carboxylic acid-(N'-phenyl-hydrazide) | 94447-18-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-methyl-1(2)H-pyrazole-3-carboxylic acid-(N'-phenyl-hydrazide)
• 英文别名: 5-Methyl-1(2)H-pyrazol-3-carbonsaeure-(N'-phenyl-hydrazid)；5-Methyl-2H-pyrazole-3-carboxylic acid, 2-phenylhydrazide；5-methyl-N'-phenyl-1H-pyrazole-3-carbohydrazide
• CAS: 94447-18-4
• 化学式: C₁₁H₁₂N₄O
• 分子量: 216.242
• InChiKey: BSFQGLDORMVAOZ-UHFFFAOYSA-N

物化性质

• 保留指数：
  2400

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  69.8
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  甲酸 、 5-methyl-1(2)H-pyrazole-3-carboxylic acid-(N'-phenyl-hydrazide) 反应 2.0h， 以90%的产率得到N-[(5-methyl-1H-pyrazole-3-carbonyl)amino]-N-phenylformamide
  参考文献：
  名称：

  Tihanyi; Feher; Gal, European Journal of Medicinal Chemistry, 1984, vol. 19, # 5, p. 433 - 439

  摘要：

  DOI：
• 作为产物：
  描述：

  5-甲基-1H-吡唑-3-羧酸 在 氯化亚砜 作用下， 生成 5-methyl-1(2)H-pyrazole-3-carboxylic acid-(N'-phenyl-hydrazide)
  参考文献：
  名称：

  Musante, Gazzetta Chimica Italiana, 1945, vol. 75, p. 121,133

  摘要：

  DOI：

文献信息

• IDO Inhibitors
  申请人：Mautino Mario

  公开号：US20110053941A1

  公开（公告）日：2011-03-03

  Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.

  目前提供以下方法：(a) 通过接触本文中描述的化合物的调节有效量与吲哚胺2,3-二氧化酶相互作用，从而调节吲哚胺2,3-二氧化酶的活性；(b) 治疗需要吲哚胺2,3-二氧化酶(IDO)介导的免疫抑制的患者，包括给予本文中描述的化合物的有效吲哚胺2,3-二氧化酶抑制剂量；(c) 治疗需要抑制吲哚胺-2,3-二氧化酶酶活性的医疗状况，包括给予本文中描述的化合物的有效吲哚胺2,3-二氧化酶抑制剂量；(d) 增强抗癌治疗的有效性，包括给予抗癌剂和本文中描述的化合物；(e) 治疗与癌症相关的肿瘤特异性免疫抑制，包括给予本文中描述的化合物的有效吲哚胺2,3-二氧化酶抑制剂量；(f) 治疗与传染病相关的免疫抑制，例如HIV-1感染，包括给予本文中描述的化合物的有效吲哚胺2,3-二氧化酶抑制剂量。
• Tihanyi, E.; Gal, M.; Feher, Oe., Journal of Heterocyclic Chemistry, 1989, vol. 26, p. 1045 - 1051
  作者：Tihanyi, E.、Gal, M.、Feher, Oe.、Dvortsak, P.

  DOI：——

  日期：——
• TIHANYI, E.;FEHER, OE.;GAL, M.;JANAKY, J.;TOLNAY, P.;SEBESTYEN, L., EUR. J. MED. CHEM., 1984, 19, N 5, 433-439
  作者：TIHANYI, E.、FEHER, OE.、GAL, M.、JANAKY, J.、TOLNAY, P.、SEBESTYEN, L.

  DOI：——

  日期：——
• Tihanyi; Feher; Gal, European Journal of Medicinal Chemistry, 1984, vol. 19, # 5, p. 433 - 439
  作者：Tihanyi、Feher、Gal、et al.

  DOI：——

  日期：——
• Musante, Gazzetta Chimica Italiana, 1945, vol. 75, p. 121,133
  作者：Musante

  DOI：——

  日期：——