Tìm theo
Cefoperazone
Các tên gọi khác (5 ) :
  • (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxo-1-piperazinylcarboxamido)-2-(4-hydroxyphenyl)acetamido)-3-((1-methyl-1H-tetrazol-5-yl)thiomethyl)-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-en-2-carbonsaeure
  • (6R,7R)-7-[[2-[(4-Ethyl-2,3-dioxopiperazine-1-carbonyl)amino]-2-(4-hydroxyphenyl)acetyl]amino]-3-[(1-methyltetrazol-5-yl)sulfanylmethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
  • Cefoperazone
  • Cefoperazono
  • Cefoperazonum
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 62893-19-0
ATC: J01DD12
ĐG : Pfizer Inc. , http://www.pfizer.com
CTHH: C25H27N9O8S2
PTK: 645.667
Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It has been proposed especially against Pseudomonas infections.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C25H27N9O8S2
Phân tử khối
645.667
Monoisotopic mass
645.142400265
InChI
InChI=1S/C25H27N9O8S2/c1-3-32-8-9-33(21(39)20(32)38)24(42)27-15(12-4-6-14(35)7-5-12)18(36)26-16-19(37)34-17(23(40)41)13(10-43-22(16)34)11-44-25-28-29-30-31(25)2/h4-7,15-16,22,35H,3,8-11H2,1-2H3,(H,26,36)(H,27,42)(H,40,41)/t15?,16-,22-/m1/s1
InChI Key
InChIKey=GCFBRXLSHGKWDP-WTKTZPJXSA-N
IUPAC Name
(6R,7R)-7-(2-{[(4-ethyl-2,3-dioxopiperazin-1-yl)carbonyl]amino}-2-(4-hydroxyphenyl)acetamido)-3-{[(1-methyl-1H-1,2,3,4-tetrazol-5-yl)sulfanyl]methyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Traditional IUPAC Name
(6R,7R)-7-{2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carbonylamino]-2-(4-hydroxyphenyl)acetamido}-3-{[(1-methyl-1,2,3,4-tetrazol-5-yl)sulfanyl]methyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
SMILES
[H][C@]12SCC(CSC3=NN=NN3C)=C(N1C(=O)[C@H]2NC(=O)C(NC(=O)N1CCN(CC)C(=O)C1=O)C1=CC=C(O)C=C1)C(O)=O
Độ tan chảy
188-190
Độ hòa tan
2.86e-01 g/l
logP
-0.74
logS
-3.4
pKa (strongest acidic)
3.38
pKa (Strongest Basic)
-1.7
PSA
220.26 Å2
Refractivity
169.06 m3·mol-1
Polarizability
62.62 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
11
H Bond Donor Count
4
Physiological Charge
-1
Number of Rings
5
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Cefoperazone is a third generation cephalosporin antibiotic. Cefoperazone exerts its bactericidal effect by inhibiting the bacterial cell wall synthesis
Cơ Chế Tác Dụng : Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It has been proposed especially against Pseudomonas infections. Like all beta-lactam antibiotics, cefoperazone binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, causing the inhibition of the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins.
Dược Động Học :

▧ Protein binding :
The degree of reversible protein binding varies with the serum concentration from 93% at 25 mcg/mL to 90% at 250 mcg/mL and 82% at 500 mcg/mL. Cefotetan is 88% plasma protein bound.
▧ Metabolism :
No significant quanitity of metabolites have been identified in urine.
▧ Route of Elimination :
Cefoperazone is excreted mainly in the bile.
▧ Half Life :
The mean serum half-life is approximately 2.0 hours, independent of the route of administration.
Độc Tính : Symptoms of overdose include blood in the urine, diarrhea, nausea, upper abdominal pain, and vomiting.
Chỉ Định : For the treatment of bacterial infections caused by susceptible microorganisms.
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Powder, for solution - Intramuscular
Powder, for solution - Intravenous
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Pfizer
    Sản phẩm biệt dược : Cefobid
  • Công ty : Pfizer
    Sản phẩm biệt dược : Cefobine
  • Công ty : Pfizer
    Sản phẩm biệt dược : Cefobis
  • Công ty : Pfizer
    Sản phẩm biệt dược : Cefoperazin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01329
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=44185
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504543
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06883
ChemSpider
http://www.chemspider.com/Chemical-Structure.40204.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0049-1201-83
PharmGKB
http://www.pharmgkb.org/drug/PA448849
Wikipedia
http://en.wikipedia.org/wiki/Cefoperazone
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