Tìm theo
Sertaconazole
Các tên gọi khác (5 ) :
  • Demofix
  • Ertaczo
  • Sertaconazol
  • Sertaconazole
  • Sertaconazolum
antifungal agents
Thuốc Gốc
Small Molecule
CAS: 99592-32-2
ATC: D01AC14
ĐG : Ortho-McNeil-Janssen Pharmaceuticals Inc. , http://www.ortho-mcneil.com
CTHH: C20H15Cl3N2OS
PTK: 437.77
Sertaconazole nitrate is an antifungal medication of the imidazole class. It is available as a cream to treat skin infections such as athlete's foot. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H15Cl3N2OS
Phân tử khối
437.77
Monoisotopic mass
435.997066923
InChI
InChI=1S/C20H15Cl3N2OS/c21-14-4-5-16(18(23)8-14)19(9-25-7-6-24-12-25)26-10-13-11-27-20-15(13)2-1-3-17(20)22/h1-8,11-12,19H,9-10H2
InChI Key
InChIKey=JLGKQTAYUIMGRK-UHFFFAOYSA-N
IUPAC Name
1-{2-[(7-chloro-1-benzothiophen-3-yl)methoxy]-2-(2,4-dichlorophenyl)ethyl}-1H-imidazole
Traditional IUPAC Name
sertaconazole
SMILES
ClC1=CC(Cl)=C(C=C1)C(CN1C=CN=C1)OCC1=CSC2=C1C=CC=C2Cl
Độ hòa tan
Practically insoluble
logP
6.2
logS
-4.8
pKa (Strongest Basic)
6.77
PSA
27.05 Å2
Refractivity
111.6 m3·mol-1
Polarizability
42.93 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Sertaconazole is an imidazole/triazole type antifungal agent. Sertaconazole is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethylation via the inhibition of the enzyme cytochrome P450 14α-demethylase. This enzyme converts lanosterol to ergosterol, and is required in fungal cell wall synthesis. The subsequent loss of normal sterols correlates with the accumulation of 14 α-methyl sterols in fungi and may be partly responsible for the fungistatic activity of fluconazole. Mammalian cell demethylation is much less sensitive to fluconazole inhibition. Sertaconazole exhibits in vitro activity against Cryptococcus neoformans and Candida spp. Fungistatic activity has also been demonstrated in normal and immunocompromised animal models for systemic and intracranial fungal infections due to Cryptococcus neoformans and for systemic infections due to Candida albicans.
Cơ Chế Tác Dụng : Sertaconazole nitrate is an antifungal medication of the imidazole class. It is available as a cream to treat skin infections such as athlete's foot. [Wikipedia] Sertaconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Sertaconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.
Dược Động Học :
▧ Absorption :
Bioavailability is negligible.
▧ Protein binding :
>99% to plasma
Chỉ Định : For the topical treatment of interdigital tinea pedis in immunocompetent patients 12 years of age and older, caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
Liều Lượng & Cách Dùng : Cream - Topical
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Ertaczo
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01153
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=65863
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507290
ChemSpider
http://www.chemspider.com/Chemical-Structure.59273.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0062-1650-03
PharmGKB
http://www.pharmgkb.org/drug/PA164748328
Wikipedia
http://en.wikipedia.org/wiki/Sertaconazole
RxList
http://www.rxlist.com/cgi/generic/ertaczo.htm
Drugs.com
http://www.drugs.com/cdi/sertaconazole.html
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