磺胺二甲嘧啶钠 | 1981-58-4

• 物质功能分类: 原料药 - 人工合成抗感染类药 - 磺胺类药及增效剂
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 磺胺二甲嘧啶钠
• 中文别名: 2-(对氨基苯磺酰胺基)-4,6-二甲嘧啶钠；N-(4,6-二甲基-2-嘧啶基)-4-氨基苯磺酰胺钠盐；2-(对氨基苯磺酰胺基)-4,6-二甲嘧啶钠盐；N-(4,6-二甲基-2-嘧啶基)-4-氨基苯磺酰钠盐；磺胺二甲异嘧啶钠；磺胺二甲嘧啶钠盐
• 英文名称: Sulfadimidinnatrium
• CAS: 1981-58-4
• 化学式: C12H14N4NaO2S
• 分子量: 301.32
• InChiKey: MNWVJNSMYXMEIX-UHFFFAOYSA-N

物化性质

• 熔点：
  >288°C (dec.)
• 溶解度：
  H2O中可溶50mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  106
• 氢给体数：
  2
• 氢受体数：
  6

安全信息

• 危险品标志：
  Xn
• 安全说明：
  S36
• 危险类别码：
  R22
• WGK Germany：
  3
• RTECS号：
  WO9300000
• 海关编码：
  2935009090
• 危险标志：
  GHS07
• 危险性描述：
  H302
• 危险性防范说明：
  P280,P305+P351+P338

制备方法与用途

生物活性

Sulfamethazine (Sulfadimethyldiazine) 是磺胺类抗感染试剂，用于畜牧业。

靶点

Bacterial

体内研究

Sulfamethazine (80 mg/kg; intravenous injection; healthy female pigs) treatment significantly reduces α, β and AUC _0->∞ , significantly increases t _1/2 α, Vd and CIB, and upon a single intramuscular administration of 80 mg/kg of Sulfamethazine the absolute bioavailability in pigs is 1.01.

Animal Model:	19 healthy female pigs (6-week-old, 4.5-6.2 kg)
Dosage:	80 mg/kg
Administration:	Intravenous injection (Pharmacokinetic study)
Result:	The half-life in distribution phase is 0.23 h and half-lifes in eliminations phase is 9.8 h. α, β and the AUC 0->∞ were significantly decreased and t 1/2 α, Vd and CIB were significantly increased, and the absolute bioavailability in pigs is 1.01.

化学性质 

白色或乳白色结晶性粉末，无臭或几乎无臭，易溶于水，略溶于乙醇。

用途 

磺胺类药，用于脑膜炎、肺炎球菌、溶血性链球菌及某些革兰氏阴性杆菌所引起的感染。

用途 

一种抗菌磺胺药，诱导CYP3A4表达，以及通过N-乙酰转移酶乙酰化

作用方式

磺胺二甲嘧啶钠属磺胺类药，在结构上类似对氨基苯甲酸(PABA)，可与PABA竞争性作用于细菌体内的二叶酸合成酶，从而阻止PABA作为原料合成细菌所需要叶酸的过程，减少了具有代谢活性的四氢叶酸的量，而后者则是细菌合成嘌吟、胸腺嘧啶核苷和脱氧核糖核酸(DNA)的必需物质，因此抑制了细菌的生长繁殖。磺胺药的作用可被PABA及其衍生物（普鲁卡因、丁卡因）所拮抗，此外脓液以及组织的分解产物的存在也起拮抗作用，因其可提供细菌生长的必需物质。

文献信息

• METHODS AND COMPOSITIONS FOR TREATING INFECTION
  申请人：UNIVERSITY OF ROCHESTER

  公开号：US20150238473A1

  公开（公告）日：2015-08-27

  Provided herein are compositions and methods for treating or preventing infection.

  本文提供了用于治疗或预防感染的组合物和方法。
• GAMMA-AAPEPTIDES WITH POTENT AND BROAD-SPECTRUM ANTIMICROBIAL ACTIVITY
  申请人：Cai Jianfeng

  公开号：US20150274782A1

  公开（公告）日：2015-10-01

  The present invention is directed to a novel class of antimicrobial agents called γ-AApeptides. The current invention provides various categories of γ-AApeptides, for example, linear γ-AApeptides, cyclic γ-AApeptides, and lipidated γ-AApeptides. γ-AApeptides of the current invention are designed to exert antimicrobial activity while being stable and non-toxic. γ-AApeptides also do not appear to lead to the development of microbial resistance in treated microorganisms. Thus, the disclosed γ-AApeptides can be used for the treatment of various medical conditions associated with pathogenic microorganisms.

  本发明涉及一种新型类别的抗微生物药物，称为γ-AA肽。当前发明提供了各种类别的γ-AA肽，例如线性γ-AA肽、环状γ-AA肽和脂质化γ-AA肽。本发明的γ-AA肽被设计为具有抗微生物活性，同时稳定且无毒。γ-AA肽似乎也不会导致被治疗微生物体内微生物产生抗药性。因此，所披露的γ-AA肽可用于治疗与病原微生物相关的各种医疗状况。
• Methods and compositions for treating infection
  申请人：UNIVERSITY OF ROCHESTER

  公开号：US10004701B2

  公开（公告）日：2018-06-26

  Provided herein are compositions and methods for treating or preventing infection.

  本文提供了用于治疗或预防感染的组合物和方法。
• γ-AApeptides with potent and broad-spectrum antimicrobial activity
  申请人：Cai Jianfeng

  公开号：US10144764B2

  公开（公告）日：2018-12-04

  The present invention is directed to a novel class of antimicrobial agents called γ-AApeptides. The current invention provides various categories of γ-AApeptides, for example, linear γ-AApeptides, cyclic γ-AApeptides, and lipidated γ-AApeptides. γ-AApeptides of the current invention are designed to exert antimicrobial activity while being stable and non-toxic. γ-AApeptides also do not appear to lead to the development of microbial resistance in treated microorganisms. Thus, the disclosed γ-AApeptides can be used for the treatment of various medical conditions associated with pathogenic microorganisms.

  本发明涉及一类名为γ-AA肽的新型抗菌剂。本发明提供了各种类型的 γ-AA肽，例如线性γ-AA肽、环状γ-AA肽和脂化γ-AA肽。本发明中的γ-AA 肽具有抗菌活性，同时稳定无毒。γ-AA肽似乎也不会导致被处理微生物产生抗药性。因此，所公开的γ-AA 肽可用于治疗与病原微生物有关的各种病症。
• Gamma-AApeptides with potent and broad-spectrum antimicrobial activity
  申请人：Cai Jianfeng

  公开号：US10308686B2

  公开（公告）日：2019-06-04

  The present invention is directed to a novel class of antimicrobial agents called γ-AApeptides. The current invention provides various categories of γ-AApeptides, for example, linear γ-AApeptides, cyclic γ-AApeptides, and lipidated γ-AApeptides. γ-AApeptides of the current invention are designed to exert antimicrobial activity while being stable and non-toxic. γ-AApeptides also do not appear to lead to the development of microbial resistance in treated microorganisms. Thus, the disclosed γ-AApeptides can be used for the treatment of various medical conditions associated with pathogenic microorganisms.

  本发明涉及一类名为γ-AA肽的新型抗菌剂。本发明提供了各种类型的 γ-AA肽，例如线性γ-AA肽、环状γ-AA肽和脂化γ-AA肽。本发明中的γ-AA 肽具有抗菌活性，同时稳定无毒。γ-AA肽似乎也不会导致被处理微生物产生抗药性。因此，所公开的γ-AA 肽可用于治疗与病原微生物有关的各种病症。