Tìm theo
Cycloserine
Các tên gọi khác (19 ) :
  • (+)-4-Amino-3-isoxazolidinone
  • (+)-Cycloserine
  • (R)-4-AMINO-isoxazolidin-3-one
  • alpha-Cycloserine
  • Cicloserina
  • cyclo-D-Serine
  • Cycloserine
  • Cycloserinum
  • D-(+)-Cycloserine
  • D-4-amino-3-Isoxazolidinone
  • D-4-amino-3-Isoxazolidone
  • D-Cycloserine
  • DCS
  • Orientomycin
  • PA 94
  • PA-94
  • Ro-1-9213
  • Seromycin
  • α-Cycloserine
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 68-41-7
ATC: J04AB01
ĐG : Eli Lilly & Co. , http://www.lilly.com
CTHH: C3H6N2O2
PTK: 102.0919
Antibiotic substance produced by Streptomyces garyphalus. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C3H6N2O2
Phân tử khối
102.0919
Monoisotopic mass
102.042927446
InChI
InChI=1S/C3H6N2O2/c4-2-1-7-5-3(2)6/h2H,1,4H2,(H,5,6)/t2-/m1/s1
InChI Key
InChIKey=DYDCUQKUCUHJBH-UWTATZPHSA-N
IUPAC Name
(4R)-4-amino-1,2-oxazolidin-3-one
Traditional IUPAC Name
cycloserine
SMILES
N[C@@H]1CONC1=O
Độ tan chảy
155.5 dec °C
Độ hòa tan
Soluble
logP
-0.9
logS
0.93
pKa (strongest acidic)
4.21
pKa (Strongest Basic)
8.36
PSA
64.35 Å2
Refractivity
21.85 m3·mol-1
Polarizability
8.87 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Cycloserine, a broad-spectrum antibiotic, may be bactericidal or bacteriostatic, depending on its concentration at the site of infection and the susceptibility of the organism. Cycloserine works by blocking the formation of these peptidoglycans. By doing this the walls of the bacteria become weak and it results in the death of the bacteria
Cơ Chế Tác Dụng : Antibiotic substance produced by Streptomyces garyphalus. [PubChem] Cycloserine is an analog of the amino acid D-alanine. It interferes with an early step in bacterial cell wall synthesis in the cytoplasm by competitive inhibition of two enzymes, L-alanine racemase, which forms D-alanine from L-alanine, and D-alanylalanine synthetase, which incorporates D-alanine into the pentapeptide necessary for peptidoglycan formation and bacterial cell wall synthesis.
Dược Động Học :
▧ Absorption :
Rapidly and almost completely absorbed (70 to 90%) from the gastrointestinal tract following oral administration.
▧ Half Life :
Half-life in patients with normal renal function is 10 hours, and is prolonged in patients with impaired renal function.
Độc Tính : Oral LD50 in mouse is 5290 mg/kg, and in rat is over 5000 mg/kg. Symptoms of a cycloserine overdose include drowsiness, confusion, headache, dizziness, irritability, numbness and tingling, difficulty speaking, paralysis, abnormal behavior, seizures, and unconsciousness.
Chỉ Định : Used in combination with up to 5 other drugs as a treatment for Mycobacterium avium complex (MAC) and is also used to treat tuberculosis (TB).
Liều Lượng & Cách Dùng : Capsule - Oral - 250 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Lilly
    Sản phẩm biệt dược : Cycloserine
  • Công ty : Merck
    Sản phẩm biệt dược : Oxamycin
  • Công ty : Lilly
    Sản phẩm biệt dược : Seromycin
  • Công ty : Lilly
    Sản phẩm biệt dược : Tisomycin
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