phenethicillin potassium | 132-93-4

• 物质功能分类: 原料药 - 抗生素类药物 - 青霉素类药
• 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: phenethicillin potassium
• 英文别名: phenethicillin potassium salt；potassium phenethicillin；potassium;N-[(2S,5R,6R)-2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptan-6-yl]-2-phenoxypropanimidate
• CAS: 132-93-4
• 化学式: C₁₇H₁₉N₂O₅S*K
• 分子量: 402.513
• InChiKey: ORMNNUPLFAPCFD-DVLYDCSHSA-M

物化性质

• 颜色/状态：
  White crystalline solid
• 溶解度：
  Very soluble in water
• 稳定性/保质期：
  DECOMP AT 230-232 °C. /DL-FORM/

计算性质

• 辛醇/水分配系数(LogP)：
  -3.25
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  124
• 氢给体数：
  1
• 氢受体数：
  6

ADMET

毒理性

• 人类毒性摘录

所有类型的皮疹...接触性皮炎...口腔病变...发热...嗜酸性粒细胞增多...间质性肾炎可能由青霉素引起。在患有潜在肾脏疾病的病人中，青霉素可能会导致异常尿沉渣或急性肾小球肾炎的肾病。/青霉素/

SKIN RASHES OF ALL TYPES...CONTACT DERMATITIS...ORAL LESIONS...FEVER... EOSINOPHILIA...INTERSTITIAL NEPHRITIS MAY...BE PRODUCED BY PENICILLINS. ... IN PT WITH UNDERLYING RENAL DISEASE, PENICILLIN MAY PRODUCE NEPHROPATHY WITH ABNORMAL URINE SEDIMENT OR ACUTE GLOMERULONEPHRITIS. /PENICILLINS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

最严重的超敏反应包括...血管神经性水肿、血清病、过敏性休克和亚急性局部反应。急性过敏性或类过敏性反应...构成了使用它们时最重要的直接危险。/青霉素类/

MOST SERIOUS HYPERSENSITIVITY REACTIONS...ARE ANGIOEDEMA, SERUM SICKNESS, ANAPHYLAXIS, & ARTHUS PHENOMENON. ... ACUTE ANAPHYLACTIC OR ANAPHYLACTOID REACTIONS...CONSTITUTE MOST IMPORTANT IMMEDIATE DANGER CONNECTED WITH THEIR USE. /PENICILLINS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

过敏反应...突然的、严重的低血压和迅速死亡。...伴有严重哮喘的支气管收缩，或腹部疼痛、恶心和呕吐，或极度虚弱和血压下降，或腹泻和紫癜样皮肤疹... /青霉素类/

ANAPHYLAXIS...SUDDEN, SEVERE HYPOTENSION & RAPID DEATH. ...BRONCHOCONSTRICTION WITH SEVERE ASTHMA, OR ABDOMINAL PAIN, NAUSEA, & VOMITING, OR EXTREME WEAKNESS & FALL IN BLOOD PRESSURE, OR DIARRHEA & PURPURIC SKIN ERUPTIONS... /PENICILLINS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

对于系统性地给予青霉素的反应很少影响眼睛，除非是继发于颅内压增加，这可能导致视乳头水肿。/青霉素/

REACTIONS TO SYSTEMICALLY ADMIN PENICILLIN HAVE RARELY AFFECTED EYES EXCEPT SECONDARILY TO INCR INTRACRANIAL PRESSURE, WHICH HAS PRODUCED PAPILLEDEMA. /PENICILLIN/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

各种皮肤疹...接触性皮炎...口腔病变...发热...嗜酸性粒细胞增多...间质性肾炎可能由青霉素引起。在患有潜在肾脏疾病的病人中，青霉素可能会导致肾病变，伴有异常尿沉渣或急性肾小球肾炎。/青霉素/

SKIN RASHES OF ALL TYPES...CONTACT DERMATITIS...ORAL LESIONS...FEVER... EOSINOPHILIA...INTERSTITIAL NEPHRITIS MAY...BE PRODUCED BY PENICILLINS. ... IN PT WITH UNDERLYING RENAL DISEASE, PENICILLIN MAY PRODUCE NEPHROPATHY WITH ABNORMAL URINE SEDIMENT OR ACUTE GLOMERULONEPHRITIS. /PENICILLINS/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

食物延缓吸收，从而延长药物的作用持续时间。口服给药后大约1小时，药物达到血浆峰浓度。

FOOD RETARDS ABSORPTION & THEREBY PROLONGS DURATION OF ACTION OF CMPD. PEAK PLASMA CONCN OCCUR ABOUT 1 HR AFTER ORAL ADMIN OF DRUG.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

口服给药时，药物吸收良好，并能逃逸酸性胃内容物的破坏；尽管如此，肠吸收仍不完全。在等量口服剂量下，它产生的血浆浓度比青霉素G或青霉素V更高。

GIVEN ORALLY, DRUG IS WELL ABSORBED & ESCAPES DESTRUCTION IN ACIDIC GASTRIC CONTENTS; DESPITE THIS FACT, INTESTINAL ABSORPTION IS INCOMPLETE. IN EQUAL ORAL DOSES, IT PRODUCES HIGHER PLASMA CONCN THAN DOES PENICILLIN G OR PENICILLIN V.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

青霉素 T/2 在人类血清中从大约25分钟增加到年轻人的2小时，在老年人中也有显著增加，这是因为肾脏小管积极分泌的药物。新生儿在等效剂量下的血清青霉素水平比儿童和成人更高，持续时间更长。/青霉素/

PENICILLIN T/2 IN HUMAN SERUM INCR FROM ABOUT 25 MIN IN YOUNG ADULTS TO 2 HR IN ELDERLY SUBJECTS & IS ALSO MARKEDLY INCR BY DRUGS WHICH ARE ACTIVELY SECRETED BY KIDNEY TUBULES. SERUM PENICILLIN LEVELS IN NEW-BORN INFANTS ARE HIGHER & MORE PROLONGED THAN IN CHILDREN & ADULTS AFTER EQUIV DOSES. /PENICILLIN/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

...迅速从体内消除，主要通过肾脏，但小部分通过胆汁和其他途径。...新生儿的清除率显著较低，因为肾功能未完全发育... /青霉素G/

...RAPIDLY ELIMINATED FROM BODY, MAINLY BY KIDNEY BUT IN SMALL PART IN BILE & BY OTHER CHANNELS. ... CLEARANCE VALUES ARE CONSIDERABLY LOWER IN NEONATES & INFANTS, BECAUSE OF INCOMPLETE DEVELOPMENT OF RENAL FUNCTION... /PENICILLIN G/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

大量出现在肝脏、胆汁、肾脏、精液、淋巴和肠道中。当脑膜正常时，青霉素不易进入脑脊液。/青霉素G/

SIGNIFICANT AMT APPEAR IN LIVER, BILE, KIDNEY, SEMEN, LYMPH, & INTESTINE. ... PENICILLIN DOES NOT READILY ENTER CSF WHEN MENINGES ARE NORMAL. /PENICILLIN G/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• WGK Germany：
  2
• RTECS号：
  XH9700000

反应信息

• 作为反应物：
  描述：

  phenethicillin potassium 生成 (Ξ)-N-((5R)-2-isopropylidene-3,7-dioxo-(5rH)-4-thia-1-aza-bicyclo[3.2.0]hept-6t-yl)-2-phenoxy-propionamide
  参考文献：
  名称：

  Anhydropenicillins: A Novel Rearrangement Of The Thiazolidine Ring

  摘要：

  DOI：

  10.1021/ja00888a039

文献信息

• FUNCTIONALLY-MODIFIED OLIGONUCLEOTIDES AND SUBUNITS THEREOF
  申请人：Sarepta Therapeutics, Inc.

  公开号：US20140330006A1

  公开（公告）日：2014-11-06

  Functionally-modified oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.

  提供了包含修改的亚单位间连接和/或修改的3'和/或5'-末端基团的功能修饰寡核苷酸类似物。所公开的化合物对于治疗需要抑制蛋白质表达或纠正异常mRNA剪接产物以产生有益治疗效果的疾病是有用的。
• Method for reducing or preventing transplant rejection in the eye and intraocular implants for use therefor
  申请人：——

  公开号：US20020182185A1

  公开（公告）日：2002-12-05

  Methods for reducing or preventing transplant rejection in the eye of an individual are described, comprising: a) performing an ocular transplant procedure; and b) implanting in the eye a bioerodible drug delivery system comprising an immunosuppressive agent and a bioerodible polymer.

  描述了减少或预防个体眼部移植排斥的方法，包括：a) 执行眼部移植手术；和b) 植入眼部一个生物可降解药物输送系统，包括免疫抑制剂和生物可降解聚合物。
• [EN] ANTIBACTERIAL QUINOLINE DERIVATIVES<br/>[FR] DÉRIVÉS DE QUINOLÉINE ANTIBACTÉRIENS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2013160435A1

  公开（公告）日：2013-10-31

  The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also 1 claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.

  本发明涉及根据一般式(Ia)或式(Ib)的新型取代喹啉衍生物：包括其任何立体化异构体、药学上可接受的盐、N-氧化物形式或溶剂化合物。所述化合物适用于治疗细菌感染。此外，还声明了包含药学上可接受的载体和所述化合物的治疗有效量作为活性成分的组合物，所述化合物或组合物用于制造治疗细菌感染药物的用途以及制备所述化合物的方法。
• ANTIBACTERIAL QUINOLINE DERIVATIVES
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：US20150065502A1

  公开（公告）日：2015-03-05

  The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.

  本发明涉及根据一般式(Ia)或式(Ib)的新型取代喹啉衍生物：包括其任何立体化异构体，其药学上可接受的盐，其N-氧化物形式或其溶剂合物。所述化合物适用于治疗细菌感染。还声明了一种包含药学上可接受的载体和所述化合物的治疗有效量作为活性成分的组合物，所述化合物或组合物用于制造治疗细菌感染的药物以及制备所述化合物的方法。
• [EN] 2-METHYLTHIOPYRROLIDINES AND THEIR USE FOR MODULATING BACTERIAL QUORUM SENSING<br/>[FR] 2-MÉTHYLTHIOPYRROLIDINES ET LEUR UTILISATION POUR MODULER LA DÉTECTION DU QUORUM BACTÉRIEN
  申请人：FLORIDA INT UNIV BOARD TRUSTEES

  公开号：WO2012174511A1

  公开（公告）日：2012-12-20

  Compounds of Formula (I) are disclosed herein and their use in inhibiting quorum sensing in bacteria.

  本文披露了化学式（I）的化合物及其在抑制细菌中的群体感应中的应用。