CAS: 77175-51-0; 1-(1-(2-((3-Chlorobenzyl)Oxy)Phenyl)Vinyl)-1H-Imidazole

该化合物是一种主要用于治疗各种真菌感染的抗风素剂,它属于伊米达佐尔衍生物类别,众所周知,这种衍生物具有抑制合成雌性激素的能力,而雌性激素是真菌细胞膜膜的临界成分,这种机制会破坏真菌细胞膜膜的完整,导致细胞死亡;克罗康那托尔展示了广泛频谱抗风素活动,使其对一系列病原体真菌有效;该物质通常根据感染的类型和严重程度进行专题或系统性管理;就物理特性而言,其特征是其水中的溶性相对较低,这可能影响其配制和交付方法;此外,在不同的环境条件下,例如光和温度,它可能表现出不同程度的稳定;安全和效能简介是其使用中的基本考虑因素,其潜在副作用可能包括局部刺激或过敏反应.

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CAS号74204-47-0 2-[1-(1H-咪唑-1-基... | CAS号620-20-2 3-氯氯苄

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    📜2-[1-(1H-咪唑-1-基)乙烯基]苯酚 反应生成 氯康唑
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    专利信息


    专利号:US-11944609-B1
    优先权日:2023-06-16
    标题:Antifungal ionic liquid and Amphotericin B combination
    发明人:RATHER SAMI-ULLAH; WANI MOHMMAD YOUNUS; BAMUFLEH HISHAM S; ALHUMADE HESHAM; SAEED USMAN; TAIMOOR AQEEL AHMAD; ALALAYAH WALID M; RATHER IRFAN AHMAD
    权利人:KING ABDULAZIZ UNIVERISTY; UNIV KING ABDULAZIZ
    摘要:Provided herein are ionic liquids that can be used as antifungal agents alone or in combination with Amphotericin B. Also disclosed are methods of synthesis of the ionic liquids and inhibiting fungal growth and methods of treating fungal infections using the disclosed compounds. The disclosure provides antifungal agents that potentiate the antifungal activity of Amphotericin B, a commonly used antifungal drug that could be used alone or in combination. This combination will help control and combat the infections caused by drug resistant Candida. auris in immunocompromised patients.

    专利号:US-9706777-B2
    优先权日:2012-05-30
    标题:Composition comprising a biological control agent and a fungicide selected from inhibitors of amino acid or protein biosynthesis, inhibitors of ATP production and inhibitors of the cell wall synthesis
    发明人:WACHENDORFF-NEUMANN ULRIKE; ANDERSCH WOLFRAM; STENZEL KLAUS; SPRINGER BERND
    权利人:BAYER CROPSCIENCE AG
    摘要:The present invention relates to a composition comprising at least one biological control agent. Furthermore, the present invention relates to the use of this composition as well as a method for reducing overall damage of plants and plant parts.

    专利号:US-2015272130-A1
    优先权日:2012-12-03
    标 题:Composition comprising a biological control agent and a fungicide
    发明人:WACHENDORFF-NEUMANN ULRIKE; DAHMEN PETER; SAWADA HARUKO
    权利人:BAYER CROPSCIENCE AG
    摘要:The present invention relates to a composition comprising at least one biological control agent selected from the group consisting of Paecilomyces lilacinus strain 251 (AGAL No. 89/030550) and Coniothyrium minitans CON/M/91-08 (DSM 9660) and/or a mutant of these strains having all the identifying characteristics of the respective strain, and/or at least one metabolite produced by the respective strain that exhibits activity against nematodes, insects and/or phytopathogens, and at least one fungicide (I) selected from the group consisting of compounds capable to introduce a host defence, inhibitors of the amino acid and/or protein biosynthesis, inhibitors of the ATP production, inhibitors of the cell wall synthesis, inhibitors of the lipid and membrane synthesis, inhibitors of the melanine biosynthesis, inhibitors of the nucleic acid synthesis, inhibitors of the signal transduction, compounds capable to act as an uncoupler, and other fungicides in a synergistically effective amount. Furthermore, the present invention relates to a kit of parts comprising said composition and the use of said composition.

    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.

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    主要参考文献


    1: El-Badry M, Fetih G, Shakeel F. Comparative topical delivery of antifungal drug croconazole using liposome and micro-emulsion-based gel formulations. Drug Deliv. 2014 Feb;21(1):34-43. doi: 10.3109/10717544.2013.843610. Epub 2013 Oct 14. 21(4):225-7. doi: 10.1111/j.1600-0536.1989.tb03200.x. 38(11-12):501-7. doi: 10.1111/j.1439-0507.1995.tb00028.x. 8(6):326-33. doi: 10.1159/000211364. 14(11):1609-13. doi: 10.1016/0731-7085(96)01777-3. 1(2):187-217. doi: 10.1128/cmr.1.2.187.
    7: Scherr N, Röltgen K, Witschel M, Pluschke G. Screening of antifungal azole drugs and agrochemicals with an adapted alamarBlue-based assay demonstrates antibacterial activity of croconazole against Mycobacterium ulcerans. Antimicrob Agents Chemother. 2012 Dec;56(12):6410-3. doi: 10.1128/AAC.01383-12. Epub 2012 Sep 24.
    8: Steinmann A, Mayer G, Breit R, Agathos M. Allergic contact dermatitis from croconazole without cross-sensitivity to clotrimazole and bifonazole. Contact Dermatitis. 1996 Oct;35(4):255-6. doi: 10.1111/j.1600-0536.1996.tb02375.x. 14(4):139-48. 8(4):211-4. doi: 10.1159/000211349.

    合成参考文献


    参考文献:10.1016/0731-7085(96)01777-3
    摘要:Akhtar MJ, Khan S, Roy IM, Jafri IA. High performance liquid chromatographic determination of phenoxetol, methyl paraben, ethyl paraben, {ce:inline-formula}n-propyl{/ce:inline-formula} paraben, {ce:inline-formula}iso-butyl{/ce:inline-formula} paraben, {ce:inline-formula}n-butyl{/ce:inline-formula} paraben and croconazole · HCl. Journal of Pharmaceutical and Biomedical Analysis. 1996 Aug;14(11):1609–13. doi: 10.1016/0731-7085(96)01777-3.
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