2-(dimethylsulfamoyl)guanidine

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机硫酸及其衍生物
• 英文名称: 2-(dimethylsulfamoyl)guanidine
• 化学式: C₃H₁₀N₄O₂S
• 分子量: 166.204
• InChiKey: UPXMQEXZZJHPFK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  盐酸胍 、 二甲胺基磺酰氯 在 碳酸氢钠 作用下， 以 丙酮 为溶剂， 反应 5.0h， 生成 2-(dimethylsulfamoyl)guanidine
  参考文献：
  名称：

  蛋白酶抑制剂：新型非碱性凝血酶抑制剂的合成和QSAR研究，该抑制剂在P1处掺入了磺酰基胍和O-甲基磺酰脲基部分。

  摘要：

  使用苯甲idine作为先导分子，已制备了两个系列的烷基/芳烷基/芳基磺酰基胍/磺酰基-O-甲基异脲+ ++，并作为两种丝氨酸蛋白酶，凝血酶和胰蛋白酶的抑制剂进行了分析。研究表明，磺胺胍及其相应的O-甲基异脲衍生物具有中等但固有的选择性凝血酶抑制特性，K（I）对凝血酶的抑制作用约为100 nM，对胰蛋白酶的抑制作用为1350-1500 nM。这两个分子的进一步加工提供了在12至50 nM范围内用K（I）抑制凝血酶的化合物，而对胰蛋白酶的亲和力仍然较低。通过将苄氧羰基或4-甲苯磺酰脲基保护的氨基酸（例如L-和D-Phe或L-Pro）或二肽（例如Phe-Pro，Gly-His，β-Ala-His，或Pro-Gly）引入上述两个导基，磺胺胍和4-氨基苯磺酰基-O-甲基异脲。因此，本研究提出了两种制备高亲和力，特异性凝血酶抑制剂的新颖方法：在已经很大的精氨酸/ am基抑制剂家族中的两个新颖的S1锚定

  DOI：

  10.1021/jm9903693

文献信息

• Cortisol secretion throughout the day, perceptions of the work environment, and negative affect
  作者：Eamonn K. S. Hanson、Cora J. M. Maas、Theo F. Meijman、Guido L. R. Godaert

  DOI：10.1007/bf02895668

  日期：2000.12

  The effects of explanatory variables derived from a work stress model (the effort-reward imbalance model) on salivary cortisol were assessed A multilevel analysis was used to distinguish the effects of single occasion and multiple occasion measurements of work stress and effect an cortisol. The single (or cross-sectional) factors include Effort-Reward imbalance (ERI), need for control negative affect, and other enduring factors (type of occupation, gender and smoking). The multiple occasion measurements include momentary negative mood, Momentary Demand-Satisfaction Ratio (MD-SR), sleep quality, work load (workday versus day off) at work (versus not being at the workplace). and lunch. The effect of time of day on cortisol was controlled for before the effects of these variables were determined.Momentary negative mood but not trait negative affect was positively associated with ambulatory measured cortisol. The variables from the work stress model-effort, reward need for control, and the multiple occasion measurements of demand arm satisfaction-did not affect cortisol. As could be expected, time of day had an effect on cortisol ,but a hypothesised interaction with momentary negative mood was not found. Additionally, the results show that the time course of cortisol differs between individuals and that the effect of sleep quality on cortisol can vary from person to person. This points to the necessity of continued efforts to single out sources of individual variability.The finding that variables derived from the effort-reward imbalance model are not related with cortisol does not support the hypothesis that ERI lends to short-term changes in cortisol, indicating no relation with hypothalamic-pituitary-adrenal (HPA) axis activity. On the other hand the present results invite further qualification of negative affect as a potential determinant of HPA activity at least, as far as can be deduced from cortisol measurements.