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曲康唑

曲康唑用途

Terconazole是用于治疗阴道酵母菌感染的广谱抗真菌药物。

曲康唑名称

[ CAS 号 ]:
67915-31-5

[ 中文名 ]:
特康唑

[ 英文名 ]:
Terconazole

[中文别名 ]:

曲康唑

[英文别名 ]:

Terconagole
MFCD05662369
Fungistat
EINECS 267-751-6
Triaconazole

曲康唑生物活性

[ 描述 ]:

Terconazole是用于治疗阴道酵母菌感染的广谱抗真菌药物。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 真菌

研究领域 >> 感染

[体外研究]

特康唑以浓度相关的方式抑制白色念珠菌ATCC 44859的生长,但当酵母在有利于细胞形式的培养基上生长时,以0.1至10μM的水平注意到适度的效应。特康唑对酵母细胞活力的抑制效力随测试的念珠菌的菌株和种类而变化。当酵母在Eagle最小必需培养基上生长时,白色念珠菌ATCC 44859对特康唑的敏感性显着增强,这有利于菌丝体的形成。存在一系列变化,从0.1μM特康唑的菌丝体形成丧失到100μM的完全坏死[1]。特康唑可以阻止形态发生从酵母转变为丝状形式,浓度为0.008至0.05微克/ mL [2]。

[体内研究]

由于阴道中延长的高生物活性抗真菌水平,每天一次3天的特曲唑唑0.8％通常足以提供7天的功能性治疗期。在任何浓度的特康唑均未观察到副作用[2]。

[动物实验]

大鼠：用白色念珠菌阴道内感染大鼠。每天两次局部治疗3天，感染后24小时开始，体积为0.2 mL各种浓度的特康唑（0.125％，0.25％，0.4％，0.5％，1％，2％），咪康唑，克霉唑，益康唑，制霉菌素或两性霉素B [2]。

[参考文献]

[1]. Tolman EL, et al. Anticandidal activities of terconazole, a broad-spectrum antimycotic. Antimicrob Agents Chemother. 1986 Jun;29(6):986-91.

[2]. Van Cutsem J, et al. The in vitro activity of terconazole against yeasts: its topical long-acting therapeutic efficacy in experimental vaginal candidiasis in rats. Am J Obstet Gynecol. 1991 Oct;165(4 Pt 2):1200-6.

[相关活性小分子]

曲康唑物理化学性质

[ 密度 ]:
1.35g/cm3

[ 沸点 ]:
681.8ºC at 760mmHg

[ 熔点 ]:
126.3ºC

[ 分子式 ]:
C₂₆H₃₁Cl₂N₅O₃

[ 分子量 ]:
532.46200

[ 闪点 ]:
366.2ºC

[ 精确质量 ]:
531.18000

[ PSA ]:
64.88000

[ LogP ]:
4.46560

[ 外观性状 ]:
粉末

[ 折射率 ]:
1.64

[ 储存条件 ]:
2-8°C

曲康唑MSDS

详细MSDS(安全技术说明书)

曲康唑安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335-H413

[ 警示性声明 ]:
P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/37/38-53

[ 安全声明 (欧洲) ]:
26

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
TL3564600

曲康唑合成路线

详细合成路线

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曲康唑文献

Azole antifungal inhibition of buprenorphine, methadone and oxycodone in vitro metabolism.

J. Anal. Toxicol. 39 , 374-86, (2015)

Opioid-related mortality rates have escalated. Drug interactions may increase blood concentrations of the opioid. We therefore used human liver microsomes (HLMs) and cDNA-expressed human cytochrome P4...

High sensitive multiresidue analysis of pharmaceuticals and antifungals in surface water using U-HPLC-Q-Exactive Orbitrap HRMS. Application to the Danube river basin on the Romanian territory.

Sci. Total Environ. 532 , 501-11, (2015)

The occurrence of 67 pharmaceutical and antifungal residues in the Danube river on the Romanian territory was studied by using solid-phase extraction (SPE) and LC-Q Exactive Orbitrap high resolution M...

Resistance status of the Colorado potato beetle, Leptinotarsa decemlineata, to endosulfan in East Azarbaijan and Ardabil provinces of Iran.

J. Insect Sci. 7 , 1-7, (2007)

Three Colorado potato beetle, Leptinotarsa decemlineata, populations, from Ardabil, Bostanabaad and Ajabshir, were collected from potato fields in East Azarbaijan and Ardabil provinces in Iran and ass...

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曲康唑