Tìm theo
Ceftobiprole
Các tên gọi khác (1) :
  • Ceftobiprole Medocaril
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 209467-52-7
CTHH: C20H22N8O6S2
PTK: 534.569
Ceftobiprole is an experimental cephalosporin antibiotic with activity against methicillin-resistant Staphylococcus aureus. It was discovered by Basilea Pharmaceutica and is being developed by Johnson & Johnson Pharmaceutical Research and Development. Ceftobiprole is the first cephalosporin to demonstrate clinical efficacy in patients with infections due to methicillin-resistant staphylococci and, if approved by regulatory authorities, is expected to be a useful addition to the armamentarium of agents for the treatment of complicated skin infections and pneumonia.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H22N8O6S2
Phân tử khối
534.569
Monoisotopic mass
534.110371856
InChI
InChI=1S/C20H22N8O6S2/c21-20-24-14(26-36-20)11(25-34)15(29)23-12-17(31)28-13(19(32)33)9(7-35-18(12)28)5-8-2-4-27(16(8)30)10-1-3-22-6-10/h5,10,12,18,22,26H,1-4,6-7H2,(H2,21,24)(H,23,29)(H,32,33)/b8-5+,14-11-/t10-,12-,18-/m1/s1
InChI Key
InChIKey=LXLDMYXULSBRCX-HZEONMFJSA-N
IUPAC Name
(6R,7R)-7-{2-[(3Z)-5-amino-2,3-dihydro-1,2,4-thiadiazol-3-ylidene]-2-nitrosoacetamido}-8-oxo-3-{[(3E)-2-oxo-1-[(3R)-pyrrolidin-3-yl]pyrrolidin-3-ylidene]methyl}-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Traditional IUPAC Name
(6R,7R)-7-{2-[(3Z)-5-amino-2H-1,2,4-thiadiazol-3-ylidene]-2-nitrosoacetamido}-8-oxo-3-{[(3E)-2-oxo-1-[(3R)-pyrrolidin-3-yl]pyrrolidin-3-ylidene]methyl}-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
SMILES
[H][C@]12SCC(\C=C3/CCN([C@@H]4CCNC4)C3=O)=C(N1C(=O)[C@H]2NC(=O)C(\N=O)=C1\NSC(N)=N1)C(O)=O
Độ hòa tan
4.78e-01 g/l
logP
-4.8
logS
-3
pKa (strongest acidic)
3.28
pKa (Strongest Basic)
10.33
PSA
198.89 Å2
Refractivity
151.2 m3·mol-1
Polarizability
50.36 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
10
H Bond Donor Count
5
Physiological Charge
0
Number of Rings
5
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Ceftobiprole, a cephalosporin antibiotic, is active against methicillin-resistant Staphylococcus aureus.
Cơ Chế Tác Dụng : Ceftobiprole is an experimental cephalosporin antibiotic with activity against methicillin-resistant Staphylococcus aureus. It was discovered by Basilea Pharmaceutica and is being developed by Johnson & Johnson Pharmaceutical Research and Development. Ceftobiprole is the first cephalosporin to demonstrate clinical efficacy in patients with infections due to methicillin-resistant staphylococci and, if approved by regulatory authorities, is expected to be a useful addition to the armamentarium of agents for the treatment of complicated skin infections and pneumonia. Cephalosporins, such as ceftobiprole, are bactericidal and have the same mode of action as other beta-lactam antibiotics (such as penicillins). Cephalosporins disrupt the synthesis of the peptidoglycan layer of bacterial cell walls. The peptidoglycan layer is important for cell wall structural integrity, especially in Gram-positive organisms. The final transpeptidation step in the synthesis of the peptidoglycan is facilitated by transpeptidases known as penicillin binding proteins (PBPs). PBPs bind to the D-Ala-D-Ala at the end of muropeptides (peptidoglycan precursors) to crosslink the peptidoglycan. Beta-lactam antibiotics mimic this site and competitively inhibit PBP crosslinking of peptidoglycan.
Chỉ Định : For the treatment of serious bacterial infections in hospitalised patients.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04918
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6918430
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=12015243
ChemSpider
http://www.chemspider.com/Chemical-Structure.5293627.html
Wikipedia
http://en.wikipedia.org/wiki/Ceftobiprole
... loading
... loading