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Sci Rep. 2016 May 18;6:26213. doi: 10.1038/srep26213.
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The biology and chemistry of antifungal agents: a review.抗真菌药物的生物学和化学：综述。
Bioorg Med Chem. 2012 Oct 1;20(19):5678-98. doi: 10.1016/j.bmc.2012.04.045. Epub 2012 May 9.
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Synthesis and antimicrobial activity of amido linked pyrrolyl and pyrazolyl-oxazoles, thiazoles and imidazoles.酰胺基连接的吡咯基和吡唑基-恶唑、噻唑和咪唑的合成及抗菌活性。
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Synthesis, characterization and antimicrobial studies of some new pyrazole incorporated imidazole derivatives.合成、表征及一些新的吡唑并咪唑衍生物的抗菌研究。
Eur J Med Chem. 2011 Aug;46(8):3531-6. doi: 10.1016/j.ejmech.2011.05.005. Epub 2011 May 12.
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Synthesis, spectral, crystal structure and in vitro antimicrobial evaluation of imidazole/benzotriazole substituted piperidin-4-one derivatives.合成、光谱、晶体结构及咪唑/苯并三唑取代的哌啶-4-酮衍生物的体外抗菌评价。
Eur J Med Chem. 2011 May;46(5):1926-34. doi: 10.1016/j.ejmech.2011.02.036. Epub 2011 Feb 23.
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Cytotoxic activity of 3-(5-phenyl-3H-[1,2,4]dithiazol-3-yl)chromen-4-ones and 4-oxo-4H-chromene-3-carbothioic acid N-phenylamides.3-(5-苯基-3H-[1,2,4]二噻唑-3-基)色烯-4-ones 和 4-氧代-4H-色烯-3-硫代羧酸 N-苯甲酰胺的细胞毒性活性。
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Mechanism of unusual formation of 3-(5-phenyl-3H-[1,2,4]dithiazol-3-yl)chromen-4-ones and 4-oxo-4H-chromene-3-carbothioic acid N-phenylamides and their antimicrobial evaluation.3-(5-苯基-3H-[1,2,4]二噻唑-3-基)色满-4-酮和4-氧代-4H-色烯-3-硫代羧酸N-苯基酰胺的异常形成机制及其抗菌活性评价
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Emergence of highly fluoroquinolone-resistant Salmonella enterica serovar Typhi in a community-based fever surveillance from Kolkata, India.在印度加尔各答开展的一项基于社区的发热监测中，出现了对氟喹诺酮高度耐药的伤寒沙门氏菌肠炎血清型菌株。
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Synthesis and antifungal activity of some new 3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl) chromones.一些新型3-羟基-2-(1-苯基-3-芳基-4-吡唑基)色酮的合成与抗真菌活性
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2-（色酮-3-基）咪唑衍生物作为潜在抗菌剂：合成、生物学评价及分子对接研究

2-(chromon-3-yl)imidazole derivatives as potential antimicrobial agents: synthesis, biological evaluation and molecular docking studies.

作者信息

Sharma Shweta, Sharma Vishal, Singh Gurpreet, Kaur Harpreet, Srivastava Shubham, Ishar Mohan Paul S

机构信息

Bio-organic and Photochemistry Laboratory, Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab -143005 India.

Department of Microbiology, Guru Nanak Dev University, Amritsar, Punjab -143005 India.

出版信息

J Chem Biol. 2016 Nov 16;10(1):35-44. doi: 10.1007/s12154-016-0162-8. eCollection 2017 Jan.

DOI:10.1007/s12154-016-0162-8
PMID:28101253
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5218924/
Abstract

A series of novel 2-(chromon-3-yl)-4,5-diphenyl-1-imidazoles (-) were synthesized by one pot condensation of substituted 3-formylchromones (-), benzil (2) and ammonium acetate (3) in refluxing acetic acid at 110 °C under N2 atmosphere. Allylation of compounds - with allyl bromide in the presence of fused KCO furnished allyl2-(chromon-3-yl)-4,5-diphenyl-1-imidazoles (-). The synthesized compounds were characterized spectroscopically and evaluated for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains by disc diffusion method. Compounds bearing electron withdrawing substituents such as () showed significant inhibitory activity against . (MIC 1.4 μg/ml) and containing substituent, displayed more inhibitory potential against . (MIC 1.5), as compared to the standard drugs. Compounds and exhibit remarkable inhibitory potential against . with MIC 0.98 and 1.23, respectively. The time kill assay for active compound was performed by viable cell count (VCC) method to elucidate the microbicidal nature of 2-(chromon-3-yl)imidazoles. A molecular docking study of most active compounds with target 'lanosterol 14α-demethylase' (CYP51) was performed to unravel the mode of antifungal action.

摘要

在氮气氛围下，于110℃的回流乙酸中，通过取代的3 - 甲酰基色酮（-）、联苯甲酰（2）和乙酸铵（3）一锅法缩合反应，合成了一系列新型的2 -（色酮 - 3 - 基）- 4,5 - 二苯基 - 1 - 咪唑（-）。在熔融碳酸钾存在下，化合物 - 与烯丙基溴进行烯丙基化反应，得到烯丙基2 -（色酮 - 3 - 基）- 4,5 - 二苯基 - 1 - 咪唑（-）。通过光谱对合成的化合物进行了表征，并采用纸片扩散法对其针对各种致病细菌和真菌菌株的体外抗菌活性进行了评估。带有吸电子取代基如（）的化合物对（MIC 1.4μg/ml）显示出显著的抑制活性，而含有取代基的化合物对（MIC 1.5）显示出比标准药物更强的抑制潜力。化合物和对（MIC分别为0.98和1.23）表现出显著的抑制潜力。通过活菌计数（VCC）方法对活性化合物进行了时间杀菌试验，以阐明2 -（色酮 - 3 - 基）咪唑的杀菌性质。对最具活性的化合物与靶标“羊毛甾醇14α - 脱甲基酶”（CYP51）进行了分子对接研究，以揭示其抗真菌作用模式。