曲康唑
中文名称:
曲康唑
中文同义词:
曲康唑;特康唑;1-[4-[[(2R,4S)-2-(2,4-二氯苯基)-2-(1,2,4-三唑-1-基甲基)-1,3-二氧戊环-4-基]甲氧基]苯基]-4-丙-2-基哌嗪;特康唑,曲康唑;曲康唑、特康唑;特康唑杂质;特康唑 标准品;曲康唑 USP标准品
英文名称:
Terconazole
英文同义词:
TERCONAZOLE;1-[4-[[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-4-propan-2-yl-piperazine;R42470;Piperazine,1-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylMethyl)-1,3-dioxolan-4-yl]Methoxy]phenyl]-4-(1-Methylethyl)-,rel-;(+-)-1-{4-[cis-2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-ylmethoxy]phenyl}-4-isopropylpiperazine;Fungistat;Piperazine, 1-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-4-(1-methylethyl)-, cis;Terconazole (200 mg)
CAS号:
67915-31-5
分子式:
C26H31Cl2N5O3
分子量:
532.46
EINECS号:
267-751-6
相关类别:
高纯试剂;小分子抑制剂;合成抗菌药;抑制剂
Mol文件:
67915-31-5.mol
熔点
126.3°C
沸点
681.8±65.0 °C(Predicted)
密度
1.35±0.1 g/cm3(Predicted)
储存条件
Inert atmosphere,Room Temperature
溶解度
DMSO: soluble1mg/mL
酸度系数(pKa)
8.33±0.10(Predicted)
形态
powder
颜色
white
CAS 数据库
67915-31-5(CAS DataBase Reference)
性质
曲康唑属三唑类抗真菌药，易溶于三氯甲烷、几乎不溶于水。
用途
曲康唑对念珠菌、许表皮癣菌和其他真菌有抗菌作用对某些细菌也有抗菌作用；主要用于外阴阴道念珠菌病的治疗。
不良反应
对0.4%曲康唑和2%咪康唑膏的不良反应进行研究，曲康唑组皮疹、生殖道刺激、疼痛和妁热的发生率分别为1.3%、3.1%、1.2%和5.2%；咪康唑组生殖道刺激、疼痛和妁热的发生率分别为0.9%、3.1%、10.5%，咪康唑组患者未出现皮疹，有2%患者出现流涕(rhinorrhea)。比较曲康唑阴道栓80mg和咪康唑栓的不良反应情况，分别有6.3%的曲康唑组患者和0.7%咪康唑组患者用药后出现腹痛，两组患者的其他不良反应发生率相似。Hyder等(1994)报道应用曲康唑治疗VVC后患者出现发热和白细胞升高。
生物活性
Terconazole (Terazol 3, Terazol 7, Triaconazole, Gyno-Terazol)是一种新型的、广谱的、三唑抗真菌试剂，主要用于治疗阴道真菌感染。
体外研究
Terconazole inhibits the growth of Candida albicans ATCC 44859 in a concentration-related manner, but with modest effects noted at levels from 0.1 to 10 μM when the yeast is grown on media favoring the cell form. The inhibitory potency of terconazole on yeast cell viability varies with the strain and species of Candida tested. The susceptibility of C. albicans ATCC 44859 to terconazole is markedly enhanced when the yeast is grown on Eagle minimum essential medium, which favors mycelium formation. There is a progression of changes, from loss of mycelia formation at 0.1 μM terconazole through complete necrosis at 100 μM. Terconazole blocks the morphogenetic transformation from the yeast into the filamentous form at concentrations of 0.008 to 0.05 microgram/mL.
体内研究
A 3-day once-daily intravaginal application of terconazole 0.8% is usually sufficient to provide a functional therapeutic period of 7 days because of prolonged high biologically active antifungal levels in the vagina. No side effects are observed at any concentration of terconazole.
危险品标志
Xi
危险类别码
36/37/38-53
安全说明
26
WGK Germany
3
RTECS号
TL3564600
海关编码
2934990002
