N-[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]acetamide | 254888-30-7

• 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: N-[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]acetamide
• CAS: 254888-30-7
• 化学式: C₁₁H₁₉NO₃
• 分子量: 213.277
• InChiKey: HZXJKBSDVZRABD-GXSJLCMTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  58.7
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• COMPOUNDS FOR PROTEASOME ENZYME INHIBITION
  申请人：Onyx Therapeutics, Inc.

  公开号：EP3101026A1

  公开（公告）日：2016-12-07

  Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

  包括含杂原子的三元环的肽基化合物能有效地、选择性地抑制 N 端亲核（Ntn）水解酶的特定活性。具有多种活性的 Ntn 的活性可受到所述化合物不同程度的抑制。例如，本发明化合物可选择性地抑制 20S 蛋白酶体的糜蛋白酶样活性。肽基化合物包括环氧化物或氮丙啶，以及 N 端的官能化。除其他治疗作用外，肽基化合物还具有抗炎和抑制细胞增殖的作用。
• Enzyme inhibition
  申请人：Crews Craig M.

  公开号：US20090099097A1

  公开（公告）日：2009-04-16

  Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.
• US7476650B2
  申请人：——

  公开号：US7476650B2

  公开（公告）日：2009-01-13