Tìm theo
AZD2563
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 252260-06-3
CTHH: C21H21F2N3O7
PTK: 465.4041
AZD2563 is an oxazolidinone antibiotic. In July 2002, after completion of phase I trials in December 2001, AstraZeneca announced that they were no longer pursuing the development of AZD2563, presumably due to negative trial results (though no results were reported).
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H21F2N3O7
Phân tử khối
465.4041
Monoisotopic mass
465.134756451
InChI
InChI=1S/C21H21F2N3O7/c22-15-7-13(26-9-14(33-21(26)30)11-31-18-3-6-32-24-18)8-16(23)19(15)12-1-4-25(5-2-12)20(29)17(28)10-27/h1,3,6-8,14,17,27-28H,2,4-5,9-11H2
InChI Key
InChIKey=HBUJYEUPIIJJOS-UHFFFAOYSA-N
IUPAC Name
3-{4-[1-(2,3-dihydroxypropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-3,5-difluorophenyl}-5-[(1,2-oxazol-3-yloxy)methyl]-1,3-oxazolidin-2-one
Traditional IUPAC Name
3-{4-[1-(2,3-dihydroxypropanoyl)-3,6-dihydro-2H-pyridin-4-yl]-3,5-difluorophenyl}-5-[(1,2-oxazol-3-yloxy)methyl]-1,3-oxazolidin-2-one
SMILES
OCC(O)C(=O)N1CCC(=CC1)C1=C(F)C=C(C=C1F)N1CC(COC2=NOC=C2)OC1=O
Độ hòa tan
7.10e-01 g/l
logP
0.78
logS
-2.8
pKa (strongest acidic)
12.4
pKa (Strongest Basic)
-1.8
PSA
125.57 Å2
Refractivity
109.52 m3·mol-1
Polarizability
44.3 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
7
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : AZD2563 is an oxazolidinone antibiotic. Oxazolidinones inhibit protein synthesis by binding at the P site at the ribosomal 50S subunit. Resistance to other protein synthesis inhibitors does not affect oxazolidinone activity, however rare development of oxazolidinone resistance cases, associated with 23S rRNA alterations during treatment have been reported.
Cơ Chế Tác Dụng : AZD2563 is an oxazolidinone antibiotic. In July 2002, after completion of phase I trials in December 2001, AstraZeneca announced that they were no longer pursuing the development of AZD2563, presumably due to negative trial results (though no results were reported). AZD2563 selectively inhibits bacterial protein synthesis through binding to sites on the bacterial ribosome and prevents the formation of a functional 70S-initiation complex. Specifically, AZD2563 binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is an essential component of the bacterial translation process.
Độc Tính : Clinical signs of acute toxicity lead to decreased activity, ataxia, vomiting and tremors.
Chỉ Định : For the treatment of gram-positive infections, including multiresistant strains.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Posizolid
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04850
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=11972575
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=10549741
ChemSpider
http://www.chemspider.com/Chemical-Structure.10145935.html
... loading
... loading