Tìm theo
Temafloxacin
Các tên gọi khác (3) :
  • Temafloxacina
  • Temafloxacine
  • Temafloxacinum
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 108319-06-8
ATC: J01MA05
CTHH: C21H18F3N3O3
PTK: 417.3811
Temafloxacin is a fluoroquinolone antibiotic drug which was withdrawn from sale in the U.S. shortly after its approval in 1992 because of serious adverse reactions resulting in three deaths. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H18F3N3O3
Phân tử khối
417.3811
Monoisotopic mass
417.130026072
InChI
InChI=1S/C21H18F3N3O3/c1-11-9-26(5-4-25-11)19-8-18-13(7-16(19)24)20(28)14(21(29)30)10-27(18)17-3-2-12(22)6-15(17)23/h2-3,6-8,10-11,25H,4-5,9H2,1H3,(H,29,30)
InChI Key
InChIKey=QKDHBVNJCZBTMR-UHFFFAOYSA-N
IUPAC Name
1-(2,4-difluorophenyl)-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
Traditional IUPAC Name
temafloxacin
SMILES
CC1CN(CCN1)C1=C(F)C=C2C(=O)C(=CN(C2=C1)C1=C(F)C=C(F)C=C1)C(O)=O
Độ hòa tan
1.44e-02 g/l
logP
-0.20
logS
-4.5
pKa (strongest acidic)
5.6
pKa (Strongest Basic)
8.76
PSA
72.88 Å2
Refractivity
104.53 m3·mol-1
Polarizability
39.7 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
6
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Temafloxacin (marketed by Abbott Laboratories as Omniflox), is a fluoroquinolone antibiotic drug which was withdrawn from sale in the U.S. shortly after its approval in 1992 because of serious adverse reactions resulting in three deaths. Flouroquinolones such as lomefloxacin possess excellent activity against gram-negative aerobic bacteria such as E.coli and Neisseria gonorrhoea as well as gram-positive bacteria including S. pneumoniae and Staphylococcus aureus. They also posses effective activity against shigella, salmonella, campylobacter, gonococcal organisms, and multi drug resistant pseudomonas and enterobacter.
Cơ Chế Tác Dụng : Temafloxacin is a fluoroquinolone antibiotic drug which was withdrawn from sale in the U.S. shortly after its approval in 1992 because of serious adverse reactions resulting in three deaths. [Wikipedia] The bactericidal action of temafloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Dược Động Học :
▧ Absorption :
Studies in healthy volunteers indicate that the average bioavailability of temafloxacin exceeds 90%, with little intersubject variability.
▧ Metabolism :
Hepatic.
▧ Half Life :
Approximately 8 hours in patients with normal renal function.
Độc Tính : Severe adverse reactions, including allergic reactions and hemolytic anemia, developed in about fifty patients during the first four months of its use, leading to three patient deaths
Chỉ Định : For the treatment of lower respiratory tract infections, genital and urinary infections like prostatitis, and skin infections.
Tương Tác Thuốc :
  • Calcium Formation of non-absorbable complexes
  • Iron Dextran Formation of non-absorbable complexes
  • Magnesium Formation of non-absorbable complexes
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Omniflox
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01405
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60021
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508032
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02469
ChemSpider
http://www.chemspider.com/Chemical-Structure.54143.html
Wikipedia
http://en.wikipedia.org/wiki/Temafloxacin
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