CAS: 27220-47-9; 1-(2-((4-Chlorobenzyl)Oxy)-2-(2,4-Dichlorophenyl)Ethyl)-1H-Imidazole

该化合物是一种属于伊米达佐类化合物的抗冻剂,主要用于治疗各种真菌感染;它表现出对皮肤素,酵母和一些模子的广泛抗风素抗风素活动,抑制了对肉类细胞膜的重要成分 ----雌性激素的合成;这种干扰导致膜渗透性增加,最终导致细胞死亡; 蛋黄质通常是一种局部应用的热液奶油,润滑剂或粉末,使运动家脚,环虫和直线丝虫等条件有效; 其特征是水中的溶性相对较低,在皮肤上施用时提高了其功效; 此外,它具有中度的亲脂性,可以更好地穿透皮肤屏障; 蛋白质一般被很好地调和在使用时系统吸收程度极低,但局部的刺激可能发生. 其化学结构包括1H-氨基环,有助于其宝贵的化学治疗.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

2,2',4'-trichloroacetophenone 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanone 1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethan-1-ol 2,4-dichlorophenacyl bromide1-[2,4-Dichloro-β-(p-chlorobenzyloxy)phenethyl]-3-(p-fluorophenacyl)imidazolium chloride (S)-1-(2-((4-chlorobenzyl)oxy)-2-(2,4-dichlorophenyl)ethyl)-1H-imidazole (R)-1-[2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]-1H-imidazole

合成工艺路线路线简述

    2'-(1H-咪唑-1-基)-2,4-二氯苯乙酮置于sodium Tetrahydroborate,Sodium Hydride体系中,用 甲醇,N,N-二甲基甲酰胺 用作溶剂,化学反应 4.5H,反应生成益康唑
    参考文献:具有丁酰胆碱酯酶 (Buche) 和吲哚胺 2,3-双加氧酶 1 (Ido1) 抑制作用的多靶标配体 (Mtdl) 的研究:针对阿尔茨海默病的咪康唑类似物的设计和合成
    标题:具有丁酰胆碱酯酶 (Buche) 和吲哚胺 2,3-双加氧酶 1 (Ido1) 抑制作用的多靶标配体 (Mtdl) 的研究:针对阿尔茨海默病的咪康唑类似物的设计和合成
    摘要:在我们努力开发用于治疗阿尔茨海默病的有效多靶点配体的过程中,确定咪康唑显示出 Buche-Ido1 双靶点抑制作用.Morris水迷宫试验表明咪康唑能明显改善东莨菪碱损伤的认知功能.此外,它在初级肝毒性评估中显示出非常好的安全性.基于这些结果,我们设计,合成并评估了一系列咪康唑衍生物作为 Buche-Ido1 双靶点抑制剂.在12种化合物中,5I和5J在酶促评价中表现出最好的效力,因此被选择用于随后的行为研究,其中这两种化合物的作用比他克林大得多.同时,5I和5J无明显肝毒性.结果表明,咪康唑类似物为进一步开发针对阿尔茨海默病的新型 Buche-Ido1 双靶点抑制剂提供了一个有吸引力的起点.
    Doi:10.1016/j.Bmc.2018.02.014

    海关参考信息

    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:WO-2025085030-A1
    优先权日:2023-10-18
    标 题:Synthesis of semisynthetic penicillin derivatives containing hydrazone-derived thiazolidine and imidazole ring
    发明人:SARIPINAR EMIN; BURAN SUMEYYE
    权利人:ERCIYES UNIV
    摘要:The present invention relates to the novel semi-synthetic thiazolidine and imidazole penicillin, pharmaceutically acceptable derivatives thereof and their synthesis method that may cause biologically significant changes by the N-acylation reaction of 6-aminopenicillanic (6-APA) using new trisubstituted thiazolidine and imidazole acetyl chloride derivatives. The invention also relates to pharmaceutical compositions comprising these compounds and their use for therapeutic treatment in the human or animal body.

    专利号:US-8557979-B2
    优先权日:2004-06-10
    标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
    发明人:CHOI WOO-BAEG; KOWALIK EWA
    权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
    摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

    专利号:WO-2025085026-A1
    优先权日:2023-10-18
    标 题:Synthesis of semisynthetic penicillin derivatives containing hydrazone-derived thiazolidine and imidazole ring
    发明人:SARIPINAR EMIN; BURAN SUMEYYE
    权利人:T C ERCIYES UNIV
    摘要:The present invention relates to the novel semi-synthetic thiazolidine and imidazole penicillin, pharmaceutically acceptable derivatives thereof and their synthesis method that may cause biologically significant changes by the N-acylation reaction of 6-aminopenicillanic (6-APA) using new trisubstituted thiazolidine and imidazole acetyl chloride derivatives. The invention also relates to pharmaceutical compositions comprising these compounds and their use for therapeutic treatment in the human or animal body.

    专利号:US-6264962-B1
    优先权日:1997-12-19
    标 题:Use of cinnamic acid or of at least one of its derivatives in a cosmetic composition
    发明人:BRETON LIONEL; GIRERD FLORENCE; RENAULT BEATRICE
    权利人:OREAL
    摘要:The invention relates to the use of cinnamic acid, or of at least one of its derivatives, in a cosmetic composition as an agent for promoting the synthesis of the skin's total lipids. n The invention also relates to a cosmetic composition comprising an effective amount of cinnamic acid or of at least one of its derivatives.

    专利号:US-2024336559-A1
    优先权日:2021-10-06
    标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids
    发明人:OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA
    权利人:UNIV NEW YORK STATE RES FOUND
    摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.
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    主要参考文献


    1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Econazole. 2024 Nov 15. 25(1):53. doi: 10.1186/s40360-024-00779-x.
    3: De Jesús-Pérez JJ, Gabrielle M, Raheem S, Fluck EC, Rohacs T, Moiseenkova- Bell VY. Structural mechanism of TRPV5 inhibition by econazole. Structure. 2024 Feb 1;32(2):148-156.e5. doi: 10.1016/j.str.2023.11.012. Epub 2023 Dec 22.
    4: Bayan MF, Chandrasekaran B, Alyami MH. Development and Characterization of Econazole Topical Gel. Gels. 2023 Nov 25;9(12):929. doi: 10.3390/gels9120929.

    合成参考文献


    参考文献:10.1093/mutage/ger045
    摘要:Fellows MD, Doherty AT, Priestley CC, Howarth V, O'Donovan MR. The ability of the mouse lymphoma TK assay to detect aneugens. Mutagenesis. 2011 Nov;26(6):771–81. doi: 10.1093/mutage/ger045.
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