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120788-07-0

中文名稱 硫培南
英文名稱 Sulopenem
CAS 120788-07-0
分子式 C12H15NO5S3
分子量 349.45
MOL 文件 120788-07-0.mol
更新日期 2024/09/26 11:36:51
120788-07-0 結(jié)構(gòu)式 120788-07-0 結(jié)構(gòu)式

基本信息

中文別名
硫培南
硫陪南
英文別名
CP-70429
Sulopenem
CP-65207-S
Sulopenem USP/EP/BP
(S)-3-[[(5R)-2-Carboxy-6β-[(R)-1-hydroxyethyl]-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-2-en-3-yl]thio]tetrahydrothiophene 1-oxide
(5R,6S)-6-[(1R)-1-Hydroxyethyl]-7-oxo-3-[[(1R,3S)-tetrahydro-1-oxido-3-thienyl]thio]-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
4-Thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, 6-[(1R)-1-hydroxyethyl]-7-oxo-3-[[(1R,3S)-tetrahydro-1-oxido-3-thienyl]thio]-, (5R,6S)-
所屬類別
原料藥:β-內(nèi)酰胺酶抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)693.1±55.0 °C(Predicted)
密度1.74±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
酸度系數(shù)(pKa)3.88±0.40(Predicted)
形態(tài)Solid
顏色White to yellow

常見(jiàn)問(wèn)題列表

用途

硫培南是一種具有口服活性的腸胃外青霉烯類抗生素,對(duì)革蘭氏陽(yáng)性菌和革蘭氏陰性菌具有廣譜活性。它可用于尿路感染和腹腔內(nèi)感染的研究,它對(duì)銅綠假單胞菌和嗜黃單胞菌的嗜麥芽孢桿菌無(wú)效。

靶點(diǎn)

MIC: 0.015-0.12?μg/mL ( E. coli )

體外研究

Sulopenem has the potential for uncomplicated and complicated urinary tract infections and intra-abdominal infections treatment, including multidrug-resistant (MDR) infections and infections attributable to quinolone-nonsusceptible and/or extended-spectrum β-lactamase (ESBL)-producing Gram-negative bacilli.
Sulopenem inhibits the growth of most isolates of aerobic and anaerobic Gram-positive and Gram-negative bacteria, including methicillin-susceptible Staphylococcus aureus , Streptococcus pneumoniae (penicillin-susceptible and -resistant isolates), group A and B β-hemolytic streptococci, Listeria monocytogenes , Enterobacteriaceae , Haemophilus influenzae , and Moraxella catarrhalis but excluding P. aeruginosa and Stenotrophomonas maltophilia , at a concentration of ≤1?μg/mL.

體內(nèi)研究

The protective effects of Sulopenem in murine experimental systemic infections are superior to those of Imipenem/Cilastatin. In murine experimental mixed infection with Escherichia coli and Bacteroides fragilis , Sulopenem has lower ED 50 . In guinea pigs experimental lung infection with Klebsiella pneumoniae , Sulopenem is more effective than CZON or Cefotiam.

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