CAS: 119006-77-8; 1-((2-Fluorophenyl)(4-Fluorophenyl)(Phenyl)Methyl)-1H-Imidazole

该化合物是一种合成的二氮衍生物,其抑制作用主要用于治疗表面的细微微粒子,主要用于治疗表面的细微粒子,其作用机制包括抑制egosterol生物合成物,破坏真菌细胞膜的完整性.氟硝酸盐显示出对抗皮肤,酵母(如Candidaspp.)和霉子的功效,许多菌株的抑制浓度(MICs.)较低.复合物表现出有利的药用植物特性,包括按主题应用时有限的系统吸收,减少不良效应的风险.其脂质性质在保持局部作用的同时会增加皮肤渗透.氟硝酸盐因其制剂稳定性和低刺激潜力而特别突出,因此适合长期用于皮肤菌菌感染.

结构式图片

欧盟法规

C&L通报

上下游产品

CAS号342-24-5 2-氟二苯甲酮 | CAS号128092-72-8 (2-氟苯基)(4-氟苯基)(苯基)甲醇 | CAS号460-00-4 对氟溴苯 | CAS号288-32-4 咪唑 | CAS号128092-75-1 1-[氯(4-氟苯基)苯甲基]-2-氟苯

合成工艺路线路线简述

    对溴氟苯置于氯化亚砜,Magnesium,三乙胺体系中,用 乙腈 用作溶剂,化学反应 10.0H,反应生成氟曲马唑
    参考文献:Bartroli; Alguero; Boncompte,Arzneimittel-Forschung/drug Research,1992,Vol. 42,# 6,P. 832-835
    标题:Bartroli; Alguero; Boncompte,Arzneimittel-Forschung/drug Research,1992,Vol. 42,# 6,P. 832-835

    海关参考信息

    专利信息


    专利号:WO-2009056955-A1
    优先权日:2007-10-30
    标题 :Amine-bearing phospholipids (abps), their synthesis and use
    发明人:ZUMBUEHL ANDREAS
    权利人:UNIV BASEL; ZUMBUEHL ANDREAS
    摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.

    专利号:US-7199128-B2
    优先权日:2005-02-02
    标题 :8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
    发明人:BRADBURY BARTON J; WILES JASON ALLAN; DESHPANDE MILIND; WANG QIUPING; HASHIMOTO AKIHIRO; LUCIEN EDLAINE
    权利人:ACHILLION PHARMACEUTICALS INC
    摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.

    专利号:US-2009012071-A1
    优先权日:2007-04-23
    标 题 :4-substituted-1h-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2h,9h)-diones and related compounds as anti-infective agents
    发明人:BRADBURY BARTON JAMES; DESHPANDE MILIND; HASHIMOTO AKIHIRO; KIM HA YOUNG; LUCIEN EDLAINE; PAIS GODWIN; PUCCI MICHAEL JOHN; WANG QIUPING; WILES JASON ALLAN
    权利人:ACHILLION PHARMACEUTICALS INC
    摘要:The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound as the only active agent or in combination with one or more other active agents. The invention provides methods for treating or preventing microbial infections, preferably animals, by administering an effective amount of a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound to an organism suffering from or susceptible to microbial infection. The invention also provides methods of inhibiting microbial growth and survival by applying an effective amount of a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound.

    专利号:US-8946422-B2
    优先权日:2005-07-27
    标题:8-methoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones and related compounds as anti-infective agents
    发明人:BRADBURY BARTON JAMES; WILES JASON ALLAN; WANG QIUPING; HASHIMOTO AKHIRO; LUCIEN EDLAINE; PAIS GODWIN CLARENCE GILROY; DESHPANDE MILIND; PUCCI MICHEAL JOHN; KIM HA YOUNG
    权利人:BRADBURY BARTON JAMES; WILES JASON ALLAN; WANG QIUPING; HASHIMOTO AKHIRO; LUCIEN EDLAINE; PAIS GODWIN CLARENCE GILROY; DESHPANDE MILIND; PUCCI MICHEAL JOHN; KIM HA YOUNG; ACHILLION PHARMACEUTICALS INC
    摘要:The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

    专利号:US-7659399-B2
    优先权日:2005-01-05
    标 题 :1-thia-2,4a-diaza-cyclopenta[b]napththalene-3,4-diones and related compounds as anti-infective agents
    发明人:BRADBURY BARTON JAMES; WILES JASON ALLAN
    权利人:ACHILLION PHARMACEUTICALS INC
    摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

    专利号:WO-2020123881-A1
    优先权日:2018-12-12
    标题:Boron containing compounds and their uses
    发明人:LIU CHUN YU; ZHOU YASHEEN; YANG STEPHEN; LIU CBUNLIANG; ZHANG YONG-KANG
    权利人:BORAGEN INC
    摘要:The present disclosure relates to boron-containing compounds, novel combiantions, and novel uses. The disclosure provides novel benzoxaborole compounds, pharmaceutical compositions, and associated methods of use. In particular, modeling suggests the benzoxaborole compounds disclosed herein are useful for inhibiting protein prenylation or ergosterol synthesis in a pathogenic microorganism. The benzoxaborole compounds according to the disclosure are further useful for the treatment of infectious microorganisms including pathogenic fungi and protozoan parasites, such as those that cause malaria.
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    主要参考文献


    1: Alomar A, Videla S, Delgadillo J, Gich I, Izquierdo I, Forn J. Flutrimazole 1% dermal cream in the treatment of dermatomycoses: a multicentre, double-blind, randomized, comparative clinical trial with bifonazole 1% cream. Efficacy of flutrimazole 1% dermal cream in dermatomycoses. Catalan Flutrimazole Study Group. Dermatology. 1995;190(4):295-300. [Review of the clinical efficacy of flutrimazole gel in the treatment of dandruff and/or seborrheic dermatitis.]. Rev Iberoam Micol. 1998 Mar;15(1):28-32. Spanish. Spanish. doi: 10.1111/j.1439-0507.2009.01738.x.

    合成参考文献


    参考文献:10.1157/13117723
    摘要:Monteagudo Sánchez B, León Muiños E, Cabanillas González M, Novo Rodríguez AI, Ordóñez Barrosa P. [Facial dermatophytide reaction]. An Pediatr (Barc). 2008 Apr;68(4):411–2. doi: 10.1157/13117723.
    摘要:S92 | FLUOROPHARMA | List of ~340 ATC classified fluoro-pharmaceuticals | DOI:10.5281/zenodo.5979646
    摘要:Arzneimittel-Forschung. Drug Research., 42(841), 1992 []
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