2-amino-2-ethyl-4-(methylsulfonimidoyl)butanoic acid

• 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: 2-amino-2-ethyl-4-(methylsulfonimidoyl)butanoic acid
• 化学式: C₇H₁₆N₂O₃S
• 分子量: 208.28
• InChiKey: YAFHJNXECLHMKP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  13
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  113
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Manipulating nitrosative stress to kill pathologic microbes, pathologic helminths and pathologically proliferating cells or to upregulate nitrosative stress defenses
  申请人：——

  公开号：US20030207815A1

  公开（公告）日：2003-11-06

  Mammals are treated for infections or for conditions associated with pathologically proliferating mammalian cell growth (for example certain cancers, restenosis, benign prostatic hypertrophy) by administration of a manipulator of nitrosative stress to selectively kill or reduce the growth of the microbes or helminths causing the infection or of host cells infected with the microbes or of the pathologically proliferating mammalian cells. Novel agents include &agr;-alkyl-S-alkyl-homocysteine sulfoximines wherein the &agr;-alkyl contains 2 to 8 carbon atoms, and the S-alkyl-contains 1 to 10 carbon atoms. In another invention herein, mammals in need of increased nitrosative stress defenses are treated, e.g., humans at risk for a stroke because of having had a transient ischemic attack, are treated. Treatments to increase nitrosative stress defenses include, for example, repeated administrations of low doses of manipulators of nitrosative stress so that the subject treated has increased tolerance to nitrosative stress. In still another invention, mammals are treated for protozoal infections by systemic administration of L-buthionine-S-sulfoximine and agent that increases nitrosative stress.

  哺乳动物被治疗感染或与病理增殖哺乳动物细胞生长相关的情况（例如某些癌症，再狭窄，良性前列腺增生）通过给予一种硝化应激调节剂，以选择性地杀死或减少微生物或蠕虫引起的感染或受微生物感染的宿主细胞或病理增殖的哺乳动物细胞的生长。新型药剂包括α-烷基-S-烷基-同型半胱氨酸亚砜，其中α-烷基含2至8个碳原子，S-烷基含1至10个碳原子。在本发明的另一种方法中，需要增加硝化应激防御的哺乳动物被治疗，例如，由于患有短暂性缺血性发作而处于中风风险的人类被治疗。增加硝化应激防御的治疗包括例如反复给予低剂量的硝化应激调节剂，以使受治疗的对象对硝化应激具有增加的耐受性。在另一种发明中，哺乳动物通过系统给药L-丁硫氧嘧啶和增加硝化应激的药物来治疗原虫感染。
• MANIPULATING NITROSATIVE STRESS TO KILL PATHOLOGIC MICROBES, PATHOLOGIC HELMINTHS AND PATHOLOGICALLY PROLIFERATING CELLS OR TO UPREGULATE NITROSATIVE STRESS DEFENSES
  申请人：——

  公开号：US20030096870A1

  公开（公告）日：2003-05-22

  Mammals are treated for infections or for conditions associated with pathologically proliferating mammalian cell growth (for example, certain cancers, restenosis, benign prostatic hypertrophy) by administration of a manipulator of nitrosative stress to selectively kill or reduce the growth of the microbes or helminths causing the infection or of host cells infected with the microbes or of the pathologically proliferating mammalian cells. Novel agents include &agr;-alkyl-S-alkyl-homocysteine sulfoximines wherein the &agr;-alkyl contains 2 to 8 carbon atoms, and the S-alkyl- contains 1 to 10 carbon atoms. In another invention herein, mammals in need of increased nitrosative stress defenses are treated, e.g., humans at risk for a stroke because of having had a transient ischemic attack, are treated. Treatments to increase nitrosative stress defenses include, for example, repeated administrations of low doses of manipulators of nitrosative stress so that the subject treated has increased tolerance to nitrosative stress. In still another invention, mammals are treated for protozoal infections by systemic administration of L-buthionine-S-sulfoximine and agent that increases nitrosative stress.

  哺乳动物被用于治疗感染或与病理性增殖的哺乳动物细胞生长有关的疾病（例如某些癌症、再狭窄、良性前列腺肥大），通过给予一种硝化应激的调节剂，以选择性地杀死或减少引起感染的微生物或线虫或被微生物感染的宿主细胞或病理性增殖的哺乳动物细胞的生长。新型药剂包括α-烷基-S-烷基-同型半胱氨酸磺酰亚胺，其中α-烷基含有2至8个碳原子，S-烷基含有1至10个碳原子。在本发明的另一个方案中，需要增强硝化应激防御的哺乳动物被治疗，例如因为曾经有过短暂性缺血性发作而有中风风险的人类被治疗。增强硝化应激防御的治疗包括例如重复给予硝化应激调节剂的低剂量，以使受治疗的对象对硝化应激有增强的耐受性。在另一个发明中，哺乳动物通过系统给药L-丁硫氨酸-S-磺酰亚胺和增加硝化应激的药剂来治疗原虫感染。
• Stent comprising manipulators of nitrosative stress to reduce restenosis
  申请人：Duke University

  公开号：EP1595573A2

  公开（公告）日：2005-11-16

  Restenosis is prevented by providing on a stent a manipulator of nitrosative stress which inhibits protection against nitrosative stress to selectively kill or reduce the growth of pathologically proliferating cells. The manipulator can be an inhibitor or depleter of thiol synthesis; an antitumor alkylator; a selective inhibitor of transcription or translation of an antinitrosative stress gene; a selective inhibitor of an antinitrosative stress gene product; or an agent functional to convert endogenously produced NO to NO- or NO+. The manipulator can itself also cause an increase of nitrosative stress in the pathologically proliferating mammalian cells or be accompanied by a manipulator that increases that nitrosative stress.

  通过在支架上提供亚硝酸应激操纵剂来防止再狭窄，该操纵剂可抑制对亚硝酸应激的保护，从而选择性地杀死或减少病理性增殖细胞的生长。操纵剂可以是硫醇合成的抑制剂或消耗剂；抗肿瘤烷化剂；抗亚硝酸应激基因转录或翻译的选择性抑制剂；抗亚硝酸应激基因产物的选择性抑制剂；或将内源性产生的 NO 转化为 NO- 或 NO+ 的功能剂。操纵子本身也可导致病态增殖的哺乳动物细胞中亚硝酸应激反应的增加，或与增加亚硝酸应激反应的操纵子同时使用。
• Manipulation of nitrosative stress for treating microbes and helminths
  申请人：Duke University

  公开号：EP1616564A2

  公开（公告）日：2006-01-18

  Manipulators of nitrosative stress are used to treat mammalian disease by selectively killing, or inhibiting the growth of, pathologic microbes or helminths or pathologically proliferating mammalian cells or by upregulating nitrosative stress defense mechanism. Novel agents include α-alkyl-S-alkyl-homocysteine sulfoximines wherein the α-alkyl contains 2 to 8 carbon atoms, and the S-alkyl-contains 1 to 10 carbon atoms.

  亚硝酸应激操纵剂通过选择性地杀死或抑制病态微生物或蠕虫或病态增殖的哺乳动物细胞的生长，或通过上调亚硝酸应激防御机制来治疗哺乳动物疾病。新型制剂包括α-烷基-S-烷基-高半胱氨酸亚磺酰亚胺，其中α-烷基含有 2 至 8 个碳原子，S-烷基含有 1 至 10 个碳原子。
• Anti-microbial agents derived from methionine sulfoximine analogues
  申请人：——

  公开号：US20040157802A1

  公开（公告）日：2004-08-12

  Novel antimicrobial compositions containing analogues of L-methionine-SR-sulfoximine (MSO) that are effective in treating intracellular pathogen infections are provided. Specifically, the compostions provided are MSO analogues having superior antimicrobial activity with significantly less toxicity as compared to MSO. These MSO analogues are suitable for use in treating infection in animals including primates, cows, pigs, horses, rabbits, mice, rats, cats, and dogs. Moreover, the MSO analogues are ideally suited for treating infections caused by the genus Mycobacterium. Additionally, methods for using the novel MSO analogues are also provided.

  本研究提供了含有可有效治疗细胞内病原体感染的 L-蛋氨酸-SR-亚磺酰亚胺（MSO）类似物的新型抗菌组合物。具体来说，所提供的组合物是 MSO 类似物，与 MSO 相比，其抗菌活性更强，毒性更低。这些 MSO 类似物适用于治疗动物感染，包括灵长类动物、牛、猪、马、兔、小鼠、大鼠、猫和狗。此外，MSO 类似物非常适合治疗由分枝杆菌属引起的感染。此外，还提供了使用新型 MSO 类似物的方法。