Tìm theo
Lymecycline
Các tên gọi khác (8 ) :
  • (+)-N-(5-Amino-5-carboxypentylaminomethyl)-4-dimethylamino-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxonaphthacene-2-carboxamide
  • Limeciclina
  • Lymecyclinum
  • N-Lysinomethyltetracycline
  • N(2)-(((+)-5-Amino-5-carboxypentylamino)methyl)tetracycline
  • N6-((4-(Dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-2-naphthacenecarboxamido)methyl)lysine
  • Tetracycline-L-methylene lysine
  • Tetracycline-L-methylenelysine
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 992-21-2
ATC: J01AA04
ĐG : Galderma Laboratories , http://www.galderma.com
CTHH: C29H38N4O10
PTK: 602.6328
A tetracycline with a 7-chloro substitution. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C29H38N4O10
Phân tử khối
602.6328
Monoisotopic mass
602.258793456
InChI
InChI=1S/C29H38N4O10/c1-28(42)13-7-6-9-17(34)18(13)22(35)19-14(28)11-15-21(33(2)3)23(36)20(25(38)29(15,43)24(19)37)26(39)32-12-31-10-5-4-8-16(30)27(40)41/h6-7,9,14-16,21,31,34,36-37,42-43H,4-5,8,10-12,30H2,1-3H3,(H,32,39)(H,40,41)/t14-,15-,16-,21-,28+,29-/m0/s1
InChI Key
InChIKey=AHEVKYYGXVEWNO-UEPZRUIBSA-N
IUPAC Name
(2S)-6-[({[(4S,4aS,5aS,6S,12aS)-4-(dimethylamino)-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracen-2-yl]formamido}methyl)amino]-2-aminohexanoic acid
Traditional IUPAC Name
lymecycline
SMILES
[H][C@@]12C[C@@]3([H])C(C(=O)C4=C(O)C=CC=C4[C@@]3(C)O)=C(O)[C@]1(O)C(=O)C(C(=O)NCNCCCC[C@H](N)C(O)=O)=C(O)[C@H]2N(C)C
Độ hòa tan
Soluble (at all physiological pH values)
logP
0.3
logS
-2.7
pKa (strongest acidic)
0.4
pKa (Strongest Basic)
9.5
PSA
242.98 Å2
Refractivity
154.51 m3·mol-1
Polarizability
62.88 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
13
H Bond Donor Count
9
Physiological Charge
0
Number of Rings
4
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Lymecycline is a tetracycline broad-spectrum antibiotic. It is approximately 5000 times more soluble than tetracycline base and is unique amongst tetracyclines in that it is absorbed by the "active transport" process across the intestinal wall, making use of the same fast and efficient mechanism by which carbohydrates are absorbed. It inhibits cell growth by inhibiting translation.
Cơ Chế Tác Dụng : A tetracycline with a 7-chloro substitution. [PubChem] Lymecycline inhibits cell growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. The binding is reversible in nature. Lymecycline is lipophilic and can easily pass through the cell membrane or passively diffuses through porin channels in the bacterial membrane. Cells become resistant to lymecycline by at least two mechanisms: efflux and ribosomal protection. In efflux, a resistance gene encodes a membrane protein that actively pumps lymecycline out of the cell. This is the mechanism of action of the tetracycline resistance gene on the artificial plasmid pBR322. In ribosomal protection, a resistance gene encodes a protein which binds to the ribosome and prevents lymecycline from acting on the ribosome.
Dược Động Học :
▧ Absorption :
Absorption is fast and efficient. Bioavailability is 100% following oral administration.
Độc Tính : Adverse effects include nausea, vomiting, diarrhoea, glossitis, enterocolitis, dysphagia, dermatitis, hypersensitivity reactions, proctitis, and vaginitis.
Chỉ Định : For the treatment of infections and to treat acne. It may also be used to treat urinary tract infections, gum disease, and other bacterial infections such as gonorrhea and chlamydia. Lymecycline is also used commonly as a prophylactic treatment for infection by Bacillus anthracis (anthrax). It is also effective against Yersinia pestis and malaria and is also prescribed for the treatment of Lyme disease.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Eficiclina
  • Công ty :
    Sản phẩm biệt dược : Tetralisal
  • Công ty :
    Sản phẩm biệt dược : Tetralysal
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00256
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=24757945
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505518
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D06884
ChemSpider
http://www.chemspider.com/Chemical-Structure.23501197.html
PharmGKB
http://www.pharmgkb.org/drug/PA164747190
Wikipedia
http://en.wikipedia.org/wiki/Lymecycline
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