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Journal articles on the topic 'Imidazole'

Author: Grafiati

Published: 4 June 2021

Last updated: 26 July 2025

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1

Aly, Ashraf A. "Base Catalyzed Synthesis of Novel Fused-Imidazoles from N-Vinyl-1H-imidazole." Zeitschrift für Naturforschung B 60, no. 1 (2005): 106–12. http://dx.doi.org/10.1515/znb-2005-0116.

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Syntheses of various classes of fused-imidazoles are reported. The key to their successful synthesis depends on the reaction of N-vinyl-1H-imidazole with the π-deficient compounds under basic conditions. Reaction of the target imidazole with 1,1,2,2-tetracyanoethylene and dimethyl acetylenedicarboxylate afforded pyrrolo[1,2-a]imidazoles. On the other site, reaction of the target imidazole with 2-dicyanomethyleneindane-1,3-dione, 2,3-dicyano-1,4-naphthoquinone gave indanylimidazolo- [1,2-a]azepine and imidazolo[2,1-a]phenanthridine derivatives, respectively. Under basic reaction condition, vari

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2

Ganguly, Swastika, Vatsal Vithlani, Anup Kesharwani, et al. "Synthesis, antibacterial and potential anti-HIV activity of some novel imidazole analogs." Acta Pharmaceutica 61, no. 2 (2011): 187–201. http://dx.doi.org/10.2478/v10007-011-0018-2.

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Synthesis, antibacterial and potential anti-HIV activity of some novel imidazole analogs A series of 1-(2-methyl-4-nitro-imidazol-1-yl)-3-arylaminopropan-2-ones (2a-e), 2-methyl-5-nitro-1-{2-[arylmethoxy] ethyl}-1H-imidazoles (5a-d), and N-(3-hydroxyphenyl)-2-(substituted imidazol-1-yl)alkanamides (8a-e) were synthesized with the aim to develop novel imidazole analogs with broad-spectrum chemotherapeutic properties. Title compounds were evaluated for their anti-HIV and antibacterial activities.

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3

Lipson, Victoria V., Tetiana L. Pavlovska, Nataliya V. Svetlichnaya, et al. "Novel (2-amino-4-arylimidazolyl)propanoic acids and pyrrolo[1,2-c]imidazoles via the domino reactions of 2-amino-4-arylimidazoles with carbonyl and methylene active compounds." Beilstein Journal of Organic Chemistry 15 (May 6, 2019): 1032–45. http://dx.doi.org/10.3762/bjoc.15.101.

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The unexpectedly uncatalyzed reaction between 2-amino-4-arylimidazoles, aromatic aldehydes and Meldrum’s acid has selectively led to the corresponding Knoevenagel–Michael adducts containing a free amino group in the imidazole fragment. The adducts derived from Meldrum’s acid have been smoothly converted into 1,7-diaryl-3-amino-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-ones and 3-(2-amino-4-aryl-1H-imidazol-5-yl)-3-arylpropanoic acids. The interaction of 2-amino-4-arylimidazoles with aromatic aldehydes or isatins and acyclic methylene active compounds has led to the formation of pyrrolo[1,2-c]imi

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4

Gerasimova, Elena L., Elena R. Gazizullina, Maria V. Borisova, et al. "Design and Antioxidant Properties of Bifunctional 2H-Imidazole-Derived Phenolic Compounds—A New Family of Effective Inhibitors for Oxidative Stress-Associated Destructive Processes." Molecules 26, no. 21 (2021): 6534. http://dx.doi.org/10.3390/molecules26216534.

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The synthesis of inhibitors for oxidative stress-associated destructive processes based on 2H-imidazole-derived phenolic compounds affording the bifunctional 2H-imidazole-derived phenolic compounds in good-to-excellent yields was reported. In particular, a series of bifunctional organic molecules of the 5-aryl-2H-imidazole family of various architectures bearing both electron-donating and electron-withdrawing substituents in the aryl fragment along with the different arrangements of the hydroxy groups in the polyphenol moiety, namely derivatives of phloroglucinol, pyrogallol, hydroxyquinol, in

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5

Demchenko, Sergii, Roman Lesyk, Oleh Yadlovskyi, et al. "Synthesis, Antibacterial and Antifungal Activity of New 3-Aryl-5H-pyrrolo[1,2-a]imidazole and 5H-Imidazo[1,2-a]azepine Quaternary Salts." Molecules 26, no. 14 (2021): 4253. http://dx.doi.org/10.3390/molecules26144253.

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A series of novel 3-aryl-5H-pyrrolo[1,2-a]imidazole and 5H-imidazo[1,2-a]azepine quaternary salts were synthesized in 58–85% yields via the reaction of 3-aryl-6, 7-dihydro-5H-pyrrolo[1,2-a]imidazoles or 3-aryl-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepines and various alkylating reagents. All compounds were characterized by 1H NMR, 13C NMR, and LC-MS. The conducted screening studies of the in vitro antimicrobial activity of the new quaternary salts derivatives established that 15 of the 18 newly synthesized compounds show antibacterial and antifungal activity. Synthesized 3-(3,4-dichlorohenyl)-1

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6

Aonofriesei, Florin. "Increased Absorption and Inhibitory Activity against Candida spp. of Imidazole Derivatives in Synergistic Association with a Surface Active Agent." Microorganisms 12, no. 1 (2023): 51. http://dx.doi.org/10.3390/microorganisms12010051.

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This paper’s purpose was to evaluate the interaction between three imidazole derivatives, (2-methyl-1H-imidazol-1-yl)methanol (SAM3), 1,1′-methanediylbis(1H-benzimidazole (AM5) and (1H-benzo[d]imidazol-1-yl)methanol 1-hydroxymethylbenzimidazole (SAM5) on the one hand, and sodium dodecyl sulphate (SDS) on the other, as antifungal combinations against Candida spp. Inhibitory activity was assessed using the agar diffusion method and Minimal Inhibitory Concentration (MIC) and showed moderate inhibitory activity of single imidazole derivatives against Candida spp. The mean value of MIC ranged from

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7

Zhou, Qifan, Fangyu Du, Yajie Shi, Ting Fang, and Guoliang Chen. "Synthesis and Analysis of 1-Methyl-4-Phenyl-1H-Imidazol-2-Amine." Journal of Chemical Research 42, no. 12 (2018): 608–10. http://dx.doi.org/10.3184/174751918x15414286606248.

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A practical synthetic route to an important pharmaceutical intermediate 1-methyl-4-phenyl-1H-imidazol-2-amine, via a three-step sequence involving cyclisation, hydrolysis and methylation, is reported. In the process of optimisation, a novel chemical entity was isolated and confirmed to be 2,6-diphenyl-1H-imidazo[1,2-a]imidazole by MS, 1H NMR and 13C NMR. The scale-up experiment was carried out to provide 1-methyl-4-phenyl-1H-imidazol-2-amine in 27.4% total yield.

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8

Loubidi, M., M. Lorion, A. El Hakmaoui, P. Bernard, M. Akssira, and G. Guillaumet. "One-Step Synthesis of 1H-Imidazo[1,5-a]imidazole Scaffolds and Access to their Polyheterocycles." Synthesis 51, no. 21 (2019): 3973–80. http://dx.doi.org/10.1055/s-0039-1690182.

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In this work, we continue our adventure in the chemistry of 5-5 tri-nitrogen bicycles. We disclose herein a one-step reaction to synthesize 1H-imidazo[1,5-a]imidazoles with different substituents introduced through the use of a wide range of aldehydes and isocyanides by using a Groebke–Blackburn–Bienaymé multicomponent reaction. The aim is to build a new library of 1H-imidazo[1,5-a]imidazole scaffolds. This bicycle was then modified to access new nitrogen-containing polycyclic compounds.

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9

Arduengo, Anthony J., Jens R. Goerlicha, Fredric Davidson, and William J. Marshall. "Carbene Adducts of Dimethylcadmium." Zeitschrift für Naturforschung B 54, no. 11 (1999): 1350–56. http://dx.doi.org/10.1515/znb-1999-1102.

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The first examples of carbene-cadmium complexes are reported from the reactions of a variety of imidazol-2-ylidenes or imidazolin-2-ylidenes with dimethylcadmium. Four new carbene complexes are characterized by NMR spectroscopy (1H , 13C and 113Cd). The cadmium centers are strongly shifted downfield (100 -150 ppm) by interaction with the carbenes. X-ray structures are reported for three carbene-cadmium 1:1 adducts. The cadmium centers exhibit distorted trigonal-planar geometries in which the carbene ligands have an average 18.2 pm longer bond distance to cadmium compared to the methyl groups.

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10

Mlostoń, Grzegorz, Małgorzata Celeda, Katarzyna Urbaniak, et al. "Synthesis and selected transformations of 2-unsubstituted 1-(adamantyloxy)imidazole 3-oxides: straightforward access to non-symmetric 1,3-dialkoxyimidazolium salts." Beilstein Journal of Organic Chemistry 15 (February 19, 2019): 497–505. http://dx.doi.org/10.3762/bjoc.15.43.

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Adamantyloxyamine reacts with formaldehyde to give N-(adamantyloxy)formaldimine as a room-temperature-stable compound that exists in solution in monomeric form. This product was used for reactions with α-hydroxyiminoketones leading to a new class of 2-unsubstituted imidazole 3-oxides bearing the adamantyloxy substituent at N(1). Their reactions with 2,2,4,4-tetramethylcyclobutane-1,3-dithione or with acetic acid anhydride occurred analogously to those of 1-alkylimidazole 3-oxides to give imidazol-2-thiones and imidazol-2-ones, respectively. Treatment of 1-(adamantyloxy)imidazole 3-oxides with

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11

Pranabes, Bhattacharyya, Medda Arunima, Samanta Anuva, Guchhait Nikhil, and R. Das Asish. "Silica gel-mediated microwave-assisted efficient synthesis of highly substituted imidazoles and exploration of naked eye/colorimetric sensor for anions." Journal of Indian Chemical Society Vol. 88, Jul 2011 (2011): 983–93. https://doi.org/10.5281/zenodo.5785102.

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Department of Chemistry, University of Calcutta, Kolkata-700 009, India <em>E-mail</em>: ardchem@caluniv.ac.in, ardas66@rediffmail.com <em>Manuscript received 09 November 2010, revised 29 December 2010, accepted 30 December 2010</em> Ammonium formate and silica gel have been found to be efficient reagent combination for an improved and very rapid one-pot synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazoles in excellent yields. Multicomponent condensation in the presence of solid support with operational simplicity, inexpensive reagents, high yield or products, tolerance of

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12

Ashok, S. R., and M. K. Shivananda. "Synthesis and Characterization and Antifungal Screening Studies of Some Novel Imidazole Derivatives." 1 8, no. 1 (2022): 39–43. http://dx.doi.org/10.46632/jemm/8/1/7.

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Imidazole derivatives are five-mamboed heterocyclic having nitrogen, and oxygen atoms in their ring structure and exhibiting potent as well as wide range of pharmacological activities. Current investigations of imidazole derivatives have provided information that these derivatives may have applications in antimicrobial, antifungal, antiviral, as well as antidiabitic treatments. Fen bam is an imidazole derivative developed by McNeil Laboratories in the late 1970s as a novel anxiolytic drug with an at-the-time-unidentified molecular target in the brain. The imidazole ring system is present in im

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13

Mutoh, Katsuya, Hiroki Arai, Yoichi Kobayashi, and Jiro Abe. "Photo-control of the thermal radical recombination reaction: photochromism of an azobenzene-bridged imidazole dimer." Pure and Applied Chemistry 87, no. 6 (2015): 511–23. http://dx.doi.org/10.1515/pac-2014-0910.

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AbstractAmong various kinds of photochromic compounds, bridged imidazole dimers have been known as fast photo-switch molecules. Bridged imidazole dimers have opened up various potential applications to photochromic lenses and real-time holographic displays. The optical properties of bridged imidazole dimers strongly depend on the bridging moiety to tether two imidazole rings. Therefore, the control of the bridging structure by introducing another photochromic moiety would increase the versatility of bridged imidazole dimers. In this study, we designed and synthesized a new type of the bridged

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14

Hu, Chuanjiang, Charles E. Schulz, and W. Robert Scheidt. "All high-spin (S = 2) iron(ii) hemes are NOT alike." Dalton Transactions 44, no. 42 (2015): 18301–10. http://dx.doi.org/10.1039/c5dt02795k.

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15

Skonieczny, Kamil, Jarosław Jaźwiński, and Daniel Gryko. "The Synthesis of Imidazo[1,2-f]phenanthridines, Phenanthro-[9,10-d]imidazoles, and Phenanthro[9′,10′:4,5]imidazo[1,2-f]-phenanthridines via Intramolecular Oxidative Aromatic Coupling." Synthesis 49, no. 20 (2017): 4651–62. http://dx.doi.org/10.1055/s-0036-1589053.

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A short and efficient access to phenanthro[9,10-d]imidazoles, imidazo[1,2-f]phenanthridines, and phenanthro[9′,10′:4,5]imidazo[1,2-f]phenanthridines was achieved by the action of [bis(trifluoroacetoxy)iodo]benzene (PIFA) on properly substituted tetraaryl-imidazoles. By pre-installing suitable electron-donating groups, it is possible to control the site of intramolecular oxidative aromatic coupling. In particular, by placing 3,4-dimethoxyphenyl and 3-methoxyphenyl moieties in close proximity, it was possible to direct the reaction into forming two biaryl linkages leading eventually to the form

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16

Kulhánek, Jiří, та Filip Bureš. "Imidazole as a parent π-conjugated backbone in charge-transfer chromophores". Beilstein Journal of Organic Chemistry 8 (5 січня 2012): 25–49. http://dx.doi.org/10.3762/bjoc.8.4.

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Research activities in the field of imidazole-derived push–pull systems featuring intramolecular charge transfer (ICT) are reviewed. Design, synthetic pathways, linear and nonlinear optical properties, electrochemistry, structure–property relationships, and the prospective application of such D-π-A organic materials are described. This review focuses on Y-shaped imidazoles, bi- and diimidazoles, benzimidazoles, bis(benzimidazoles), imidazole-4,5-dicarbonitriles, and imidazole-derived chromophores chemically bound to a polymer chain.

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17

El'kov, N. A., Dz N. Konshina, and V. V. Konshin. "A practical synthesis of 1-[3-(trimethoxysilyl)propyl]-1<i>H</i>-imidazole." Журнал общей химии 93, no. 4 (2023): 654–56. http://dx.doi.org/10.31857/s0044460x23040182.

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A simple and effective method for the synthesis of 1-[3-(trimethoxysilyl)propyl]-1 H -imidazole was proposed by alkylation of sodium imidazolyl obtained from imidazole and sodium hydroxide with (3-chloropropyl)trimethoxysilane at reflux in toluene for 15 h. The target imidazole was obtained with a yield of 82%.

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18

E.AJILA*, R.ANIZ K.ROY THARA BAI. "SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 1H-SUBSTITUTED 2, 4, 5- TRIPHENYL IMIDAZOLE DERIVATIVES." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 08 (2018): 7367–73. https://doi.org/10.5281/zenodo.1342750.

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<em>On the basis of various literature survey, imidazole derivatives show various activity such as antimicrobial, anti-inflammatory, analgesic, antitubercular, anticancer etc. The possible improvements in the activity can be further achieved by slight modifications in the substituents on the basic imidazole nucleus. Thus imidazole offers better pharmacodynamic characteristics. Furthermore, some imidazole drugs, at high concentrations, could exert direct inhibitory effects on membranes, without interference with sterols and sterol esters. Various recent new drugs developments in imidazole deriv

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19

Mloston, Grzegorz, and Marcin Jasiński. "Synthesis and selected transformations of 3-oxido-1H-imidazole-4-carboxamides." Collection of Czechoslovak Chemical Communications 75, no. 8 (2010): 871–85. http://dx.doi.org/10.1135/cccc2010012.

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An efficient synthesis of new N-alkyl- and N-aryl-3-oxido-1H-imidazole-4-carboxamides based on exploration of inexpensive, commercially available ethyl acetoacetate, paraformaldehyde and primary amines is described. Representative compounds were tested in selected transformations, such as ‘sulfur-transfer reaction’ leading to imidazole-2-thiones and isomerization to corresponding imidazol-2-ones. Strong intramolecular hydrogen bonding via the N-oxide function results in the reduced reactivity of 3-oxido-1H-imidazole-4-carboxamides in both reactions. Moreover, the palladium catalyzed C(2)-aryla

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20

Li, Steven A., Rebecca J. Zheng, Kenneth Sue, et al. "Discovery and Preliminary Structure-Activity Investigation of 3-Substituted-1H-imidazol-5-yl-1H-indoles with In Vitro Activity towards Methicillin-Resistant Staphylococcus aureus." Antibiotics 11, no. 10 (2022): 1450. http://dx.doi.org/10.3390/antibiotics11101450.

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Antibiotics have been the cornerstone of modern medicine saving lives by virtue of being able to cure infectious diseases and to prevent infections in those who are immune compromised. Their intense use has led to a surging increase in the incidence of antibiotic-resistant bacteria resulting in a desperate need for antibiotics with new mechanisms of action. As part of our search for new antimicrobials we have screened an in-house library of compounds and identified two 3-substituted-1H-imidazol-5-yl-1H-indoles as weak growth inhibitors (MIC 16 µg/mL) against methicillin-resistant Staphylococcu

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21

Li, Laicai, Xiao Chen, Wanfei Cai, Ming Zhang, Xiaoqin Liang, and Anmin Tian. "Theoretical research on the charge transport properties of imidazoles axial-coordinated with protoheme molecule." Journal of Theoretical and Computational Chemistry 16, no. 06 (2017): 1750049. http://dx.doi.org/10.1142/s0219633617500493.

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The charge transport properties and the stability of imidazoles with axial-coordinated protoheme molecules have been investigated by the density functional theory (DFT) at B3LYP/6-31[Formula: see text]G(d) level. With energy of each compound, we find that all heme Fe[Formula: see text] and Fe[Formula: see text] complex compounds axially coordinate the imidazoles by strong field in low-spin state. Meanwhile, binding energies were calculated, the structure feature and the frontier orbital distribution of complex compounds were also analyzed. On the basis of Marcus theory, the reorganization ener

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22

Dolensky, Bohumil, and Kenneth L. Kirk. "Preparation of (Fluoromethyl)- and (Difluoromethyl)imidazoles." Collection of Czechoslovak Chemical Communications 67, no. 9 (2002): 1335–44. http://dx.doi.org/10.1135/cccc20021335.

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2-(Fluoromethyl)- and 2-(difluoromethyl)imidazoles, and 4-(fluoromethyl)- and 4-(difluoromethyl)imidazoles have been prepared by deoxyfluorination of (hydroxymethyl)imidazole or formylimidazole precursors.

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23

Singh, Praveen, Ranjeet Kumar, and Ashish Kumar Tewari. "Hydrogen bonding framework in imidazole derivatives: Crystal structure and Hirshfeld surface analysis." European Journal of Chemistry 11, no. 1 (2020): 50–59. http://dx.doi.org/10.5155/eurjchem.11.1.50-59.1945.

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A series of imidazole derivatives (1-3) were synthesized with three component reaction among benzil, ammonium acetate and formaldehyde/aromatic aldehyde at 110 °C without a catalyst and solvent. These synthesized imidazole derivatives have shown intermolecular hydrogen bonding such as N-H···N and O-H···N. The imidazole 1 and 2 exhibited N-H···N intermolecular hydrogen bonding while imidazole 3 exhibited O-H···N intermolecular hydrogen bonding. The hydrogen bonds in imidazoles were studied by X-ray crystallography and Hirshfeld Surface Analysis at dnorm surface which show the visible red spots,

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24

Alkhafaji, Mohammed Nawfal Abdul Maged, Hutham Abd Ali Abd Al Hussain, and Dr Nagham Mahmood Aljamali. "Synthesis, Spectral, Bio Assay, Chromatographic - Studying of New Imidazole Reagents Via Three Components Reaction." NeuroQuantology 19, no. 7 (2021): 115–22. http://dx.doi.org/10.14704/nq.2021.19.7.nq21092.

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Imidazoles are part of the theophylline Reagent, found in tea leaves and coffee beans, which stimulates the central nervous system. It is found in the anti-cancer drug mercaptopurine, which fights leukemia by interfering with DNA systems. A number of prepared imidazoles, including clotrimazole, are selective inhibitors of nitric oxide synthase, which makes them interesting drug targets in inflammation, respiratory diseases and tumors of the nervous system. Other biological activities of the drug carrier imidazole relate to deregulation of the intracellular fluxes of (Ca and K) ions. Novel imid

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25

Veeraragavan, Vijayakumar, Radhakrishnan Narayanaswamy, and Rameshkumar Chidambaram. "PREDICTING THE BIODEGRADABILITY NATURE OF IMIDAZOLE AND ITS DERIVATIVES BY MODULATING TWO HISTIDINE DEGRADATION ENZYMES (UROCANASE AND FORMIMINOGLUTAMASE) ACTIVITIES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 11 (2017): 383. http://dx.doi.org/10.22159/ajpcr.2017.v10i11.20999.

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Objectives: The biodegradation pathway of substituted imidazole ring compounds has been reported to have close analogy to the histidine degradation pathway. This prompted the present study to be carried out on 12 selected imidazole and its derivatives which are 1-imidazole, 1, 2-dimethylimidazole, 1-ethyl imidazole, 2-ethyl-4-methylimidazole, 2-isopropylimidazole, 2-Isopropyl-4-nitro-1H-imidazole, 1-methylimidazole, 2-methyl-5-nitroimidazole, 2-methyl-1-vinylimidazole, 1-nitro imidazole, 1-phenyl imidazole, and 1-vinylimidazole.Methods: The imidazole and its derivatives were evaluated on the d

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26

Verma, Amita, Sunil Joshi, and Deepika Singh. "Imidazole: Having Versatile Biological Activities." Journal of Chemistry 2013 (2013): 1–12. http://dx.doi.org/10.1155/2013/329412.

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Imidazoles have occupied a unique position in heterocyclic chemistry, and its derivatives have attracted considerable interests in recent years for their versatile properties in chemistry and pharmacology. Imidazole is nitrogen-containing heterocyclic ring which possesses biological and pharmaceutical importance. Thus, imidazole compounds have been an interesting source for researchers for more than a century. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine, and nucleic acid. Being a polar and ionisable aromatic compound, it imp

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27

Sengee, Gerelt-Ireedui, Narangerel Badraa, and Young Key Shim. "Synthesis and photodynamic activity of new imidazole substituted pyropheophorbide-a derivatives." Journal of Porphyrins and Phthalocyanines 13, no. 07 (2009): 818–22. http://dx.doi.org/10.1142/s1088424609001017.

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Two new imidazole substituted chlorin derivatives, namely (4-[1-imidazolyl]-phenyl)-amide pyropheophorbide-a and (3-[1-imidazolyl]-propyl)-amide pyropheophorbide-a have been synthesized. Their cell viabilities on A549 human lung adenocarcinoma cells were investigated and compared with that of pyropheophorbide-a. According to the phototoxicity study, (4-[1-imidazolyl]-phenyl)-amide pyropheophorbide-a and (3-[1-imidazolyl]-propyl)-amide pyropheophorbide-a were found superior to pyropheophorbide-a with respect to high phototoxicity. This work demonstrates that imidazole substituted chlorin deriva

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28

Xu, Wei, Hao Yao, Xing Zhang, et al. "K2CO3 Promoted Cascade Reaction for the Preparation of 1H-Imidazol-4- yl-1-amine Derivatives." Letters in Organic Chemistry 17, no. 2 (2020): 127–32. http://dx.doi.org/10.2174/1570178616666190226144620.

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: A K2CO3 promoted efficient one pot two-step method for the preparation of 1H-imidazol-4- yl-1-amine derivatives has been developed. A series of second amines with an imidazole group were obtained with 56%-91% yields by the K2CO3 promoted amination of acetates and nitrogen deprotection of the imidazole process.

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29

Rani, Nidhi, Praveen Kumar, Randhir Singh, Damião P. de Sousa, and Prerna Sharma. "Current and Future Prospective of a Versatile Moiety: Imidazole." Current Drug Targets 21, no. 11 (2020): 1130–55. http://dx.doi.org/10.2174/1389450121666200530203247.

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Imidazole containing compounds have been a very much explored field since ancient times. Subsequently, it constitutes a significant moiety for the new drug development. A variety of compounds having imidazole moiety have been synthesized, evaluated and marketed for the treatment of various diseases such as antifungal, antiepileptic, ACE inhibitors and so on, as shown in the figure. The search for imidazole containing compounds with more selective biological potency with low side effects continues to be an active area of research in medicinal chemistry. This review is in an effort to highlight

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30

Singh, Gurvinder P., Saravanan Kaliyaperymal, and Gyanendra K. Sharma. "Microwave-assisted Solvent-free Synthesis of Some New 4-[2-(Substituted phenyl)-4, 5-diphenyl-1H-imidazole-1-yl]-1H-indoles of Biological Interest." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 34, no. 02 (2024): 253. http://dx.doi.org/10.59467/ijhc.2024.34.253.

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Solvent-free, microwave-assisted synthesis of several new indolyl imidazoles of biological importance is reported. First, indoleamine was condensed with substituted aryl aldehydes to give corresponding Schiff's bases. Then, Schiff's bases were reacted with ammonium acetate and benzil using silica gel as the solid support to yield the corresponding substituted indolyl imidazole derivatives. A comparison between the conventional approach and the microwave-assisted method is also reported in this research. All the synthesized substituted indolyl imidazole derivatives showed good antibacterial act

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31

Guthrie, J. Peter, and David C. Pike. "Hydration of acylimidazoles: tetrahedral intermediates in acylimidazole hydrolysis and nucleophilic attack by imidazole on esters. The question of concerted mechanisms for acyl transfers." Canadian Journal of Chemistry 65, no. 8 (1987): 1951–69. http://dx.doi.org/10.1139/v87-326.

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Heats of hydrolysis have been measured for three acylimidazole acetals. From these results free energies of formation in aqueous solution have been calculated for the acetals and the corresponding tetrahedral intermediates. Having free energies of formation for the tetrahedral intermediates allows a detailed analysis of the energetics of both the unobservable nucleophilic reaction of imidazole with ethyl acetate and also the observable reaction of imidazole with p-nitrophenyl acetate. pKa values of 1-(3-aminopropyl)-imidazole and 1-(2-aminoethyl)-imidazole have been determined to allow calcula

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Mlostoń, Grzegorz, Małgorzata Celeda, Marcin Jasiński, et al. "2-Unsubstituted Imidazole N-Oxides as Novel Precursors of Chiral 3-Alkoxyimidazol-2-ylidenes Derived from trans-1,2-Diaminocyclohexane and Other Chiral Amino Compounds." Molecules 24, no. 23 (2019): 4398. http://dx.doi.org/10.3390/molecules24234398.

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‘Desymmetrization’ of trans-1,2-diaminocyclohexane by treatment with α,ω-dihalogenated alkylation reagents leads to mono-NH2 derivatives (‘primary-tertiary diamines’). Upon reaction with formaldehyde, these products formed monomeric formaldimines. Subsequently, reactions of the formaldimines with α-hydroxyiminoketones led to the corresponding 2-unsubstituted imidazole N-oxide derivatives, which were used here as new substrates for the in situ generation of chiral imidazol-2-ylidenes. Upon O-selective benzylation, new chiral imidazolium salts were obtained, which were deprotonated by treatment

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Xu, Guo-Wang, Ye-Nan Wang, Hai-Bing Wang та Zhong-Long Wang. "Crystal structure ofcatena-poly[[diaquacobalt(II)]-bis[μ-5-(4-carboxyylatophenyl)picolinato]-κ3N,O2:O5;κ3O5:N,O2-[diaquacobalt(II)]-μ-1-[4-(1H-imidazol-1-yl)phenyl]-1H-imidazole-κ2N3:N3′]". Acta Crystallographica Section E Crystallographic Communications 71, № 7 (2015): m145—m146. http://dx.doi.org/10.1107/s2056989015012190.

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The asymmetric unit of the title polymeric CoIIcomplex, [Co2(C13H7NO4)2(C12H10N4)(H2O)4]n, contains a CoIIcation, a 5-(4-carboxylatophenyl)picolinate dianion, two coordination water molecules and half of 1-[4-(1H-imidazol-1-yl)phenyl]-1H-imidazole ligand. The CoIIcation is coordinated by two picolinate dianions, two water molecules and one 1-[4-(1H-imidazol-1-yl)phenyl]-1H-imidazole molecule in a distorted N2O4octahedral coordination geometry. The two picolinate dianions are related by an inversion centre and link two CoIIcations, forming a binuclear unit, which is further bridged by the imida

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Lin, Xin, Mingqiang Huang, Tingting Lu, et al. "Characterization of Imidazole Compounds in Aqueous Secondary Organic Aerosol Generated from Evaporation of Droplets Containing Pyruvaldehyde and Inorganic Ammonium." Atmosphere 13, no. 6 (2022): 970. http://dx.doi.org/10.3390/atmos13060970.

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Imidazole compounds are important constituents of atmospheric brown carbon. The imidazole components of aqueous secondary organic aerosol (aqSOA) that are generated from the evaporation of droplets containing pyruvaldehyde and inorganic ammonium are on-line characterized by an aerosol laser time-of-flight mass spectrometer (ALTOFMS) and off-line detected by optical spectrometry in this study. The results demonstrated that the laser desorption/ionization mass spectra of aqSOA particles that were detected by ALTOFMS contained the characteristic mass peaks of imidazoles at m/z = 28 (CH2N+), m/z =

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Jawaharmal, H. S. Lamba, Smita Narwal, et al. "Synthesis of Novel Imidazole Compounds and Evaluation of Their Antimicrobial Activity." Indo Global Journal of Pharmaceutical Sciences 02, no. 02 (2012): 147–56. http://dx.doi.org/10.35652/igjps.2012.18.

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Imidazoles are an important class of heterocycles and include many substances of both biological and chemical interest. Insertion of the imidazole nucleus is an important synthetic strategy in drug discovery. Imidazole drugs have broad applications in many areas of clinical medicine. These are currently used as tools in pharmacological studies. The important therapeutic properties of imidazole related drugs have encouraged the medicinal chemists to synthesize and test a large number of novel molecules. In this investigation, it was of interest to synthesize imidazole by refluxing 9, 10-phenent

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Rasajna G, Hema Latha N, Sunitha P, et al. "A Review of Synthesis, Structure Activity Relationship and Therapeutic Applications of Imidazole and Its Derivatives." Journal of Pharma Insights and Research 3, no. 1 (2025): 121–29. https://doi.org/10.69613/z6yaks23.

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Imidazole and its derivatives represent a crucial class of heterocyclic compounds with extensive applications in medicinal chemistry and drug development. The imidazole scaffold, a five-membered aromatic heterocycle containing two nitrogen atoms, exhibits unique physicochemical properties and versatile reactivity patterns that make it valuable in drug design. Modern synthetic approaches, including microwave-assisted synthesis and metal-catalyzed reactions, have enabled the efficient preparation of structurally diverse imidazole derivatives. These compounds demonstrate remarkable biological act

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Müller-Buschbaum, Klaus. "3D-[Pr(Im)3(ImH)]@ImH: Ein dreidimensionales Netzwerk mit vollständiger Stickstoffkoordination aus einer Imidazolschmelze / 3D-[Pr(Im)3(ImH)]@ImH: A Three-Dimensional Network with Complete Nitrogen Coordination Obtained from an Imidazole Melt." Zeitschrift für Naturforschung B 61, no. 7 (2006): 792–98. http://dx.doi.org/10.1515/znb-2006-0704.

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The reaction of a melt of unsubstituted imidazole with praseodymium metal yields bright green crystals of 3D-[Pr(Im)3(ImH)]@ImH. Imidazolate ligands coordinate η1 via both N atoms their 1,3 positioning within the heterocycle being responsible for the connection of praseodymium atoms. A 3-dimensional network is formed with imidazole molecules from the melt intercalated in the crystal structure. The imidazole molecules can be released and temperature dependent reversibly be exchanged with gas molecules including argon. Thus the solvent free high temperature synthesis of rare earth elements with

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38

Sultana, Shameem, and G. Shiva Kumar. "Synthesis, Antimicrobial and Antitubercular Activity of Novel Imidazole Carboxamides." Asian Journal of Chemistry 35, no. 5 (2023): 1276–82. http://dx.doi.org/10.14233/ajchem.2023.27823.

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A series of novel imidazole carboxamide derivatives (6a-j) were synthesized in moderate to good yields via the oxidative esterification of 1H-imidazole-4-cabaldehyde (1) with phenol (4) followed by the aminolysis of various substituted anilines (5a-j) in the presence of 1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene (2) (IPr, 10 mol%) and TEMPO (3) in toluene. All the compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The synthesized compounds were assessed in vitro for their antimicrobial and antitubercular potential. Among the synthesized compounds 6a, 6f and 6g ha

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Bhat, Mashooq Ahmad, Mohamed A. Al-Omar, Ahmed M. Naglah, Atef Kalmouch, and Abdullah Al-Dhfyan. "Synthesis and Characterization of Novel Biginelli Dihydropyrimidinone Derivatives Containing Imidazole Moiety." Journal of Chemistry 2019 (May 13, 2019): 1–7. http://dx.doi.org/10.1155/2019/3131879.

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Enaminone, (2E)-1-[4-(1H-imidazol-1-yl) phenyl]-4-methylpent-2-en-1-one (II) was synthesized by refluxing 1-[4-(1H-imidazol-1-yl) phenyl] ethan-1-one (I) with dimethylforamide dimethylacetal (DMF–DMA) under solvent-free condition for 12 hours. Finally, the dihydropyrimidinone derivatives containing imidazole moiety (1–15) were obtained by reacting enaminone, (2E)-1-[4-(1H-imidazol-1-yl) phenyl]-4-methylpent-2-en-1-one (II) with urea and different substituted benzaldehydes in the presence of glacial acetic acid. Dihydropyrimidinone derivatives containing imidazole moiety were synthesized in exc

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40

Štefan, Leo, Ana Čikoš, Robert Vianello, Ivica Đilović, Dubravka Matković-Čalogović, and Miljenko Dumić. "Chemistry of Spontaneous Alkylation of Methimazole with 1,2-Dichloroethane." Molecules 26, no. 22 (2021): 7032. http://dx.doi.org/10.3390/molecules26227032.

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Spontaneous S-alkylation of methimazole (1) with 1,2-dichloroethane (DCE) into 1,2-bis[(1-methyl-1H-imidazole-2-yl)thio]ethane (2), that we have described recently, opened the question about its formation pathway(s). Results of the synthetic, NMR spectroscopic, crystallographic and computational studies suggest that, under given conditions, 2 is obtained by direct attack of 1 on the chloroethyl derivative 2-[(chloroethyl)thio]-1-methyl-1H-imidazole (3), rather than through the isolated stable thiiranium ion isomer, i.e., 7-methyl-2H, 3H, 7H-imidazo[2,1-b]thiazol-4-ium chloride (4a, orthorhombi

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Yang, Zunhua, Yuanying Fang, Jae-Min Kim, Kyung-Tae Lee, and Haeil Park. "Synthesis of Halogenated 1,5-Diarylimidazoles and Their Inhibitory Effects on LPS-Induced PGE2 Production in RAW 264.7 Cells." Molecules 26, no. 20 (2021): 6093. http://dx.doi.org/10.3390/molecules26206093.

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A series of halogenated 1,5-diarylimidazole compounds were synthesized and their inhibitory effects on LPS-induced PGE2 production in RAW 264.7 cells were evaluated. A wide variety of 2,4-, 4-, and 2-halogenated 5-aryl-1-(4-methylsulfonylphenyl)imidazoles were synthesized for SAR study via two different pathways. Overall, 4-halogenated 5-aryl-1-(4-methylsulfonylphenyl)imidazoles, regardless of the species of halogen, exhibited very strong inhibitory activities of PGE2 production. Among them, 4-chloro-5-(4-methoxyphenyl)-1-(4-methylsulfonylphenyl)imidazole (3, IC50 3.3 nM ± 2.93), and 4-chloro-

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Yakovychuk, N. D., S. Y. Deyneka, A. M. Grozav, A. V. Humenna, V. B. Popovych та V. S. Djuiriak. "Аntifungal activity of 5-(2-nitrovinyl) imidazoles and their derivatives against the causative agents of vulvovaginal candidiasis". Regulatory Mechanisms in Biosystems 9, № 3 (2018): 369–73. http://dx.doi.org/10.15421/021854.

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Development of resistance of yeast-like fungi belonging to the Candida genus to the existing antifungal medicines as well as the high toxicity and low tolerance of these medicines in many cases stipulate the acute need for new antibiotic compounds. In this context, an extremely promising group of chemical substances is imidazole derivatives. Therefore, the search for more active and less toxic medical preparations based on imidazole is a relevant and important issue for medical practice. Considering the urgent demand for new antifungal preparations, four new nitro containing imidazole derivati

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Gupta, A. K., A. Jain, S. Mishra, and A. Jiaswal. "Design and Synthesis of Substituted Imidazole Derivatives as Antifungal Agents." International Journal of Drug Design and Discovery 3, no. 4 (2025): 943–54. https://doi.org/10.37285/ijddd.3.4.9.

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In the present study, we have designed, predicted, synthesized and evaluated some new substituted imidazoles derivatives as antifungal agents. Here, a set of 26 substituted imidazole derivatives were investigated for molecular modeling studies using a combination of various molecular descriptors. A sequential multiple linear regression (SQMLR) procedure was used to model the relationships between molecular descriptors and the antifungal activity of the substituted imidazole derivatives. The QSAR analysis of the imidazole analogues furnished topology of molecules and electronic contribution are

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Rani, Nidhi, Praveen Kumar та Randhir Singh. "Molecular Modeling Studies of Halogenated Imidazoles against 14α- Demethylase from Candida Albicans for Treating Fungal Infections". Infectious Disorders - Drug Targets 20, № 2 (2020): 208–22. http://dx.doi.org/10.2174/1871526519666181130101054.

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Background:Imidazole is one of the most explored and marketed azole utilized for the treatment of fungal infections. Lanosterol 14α-demethylase (Cytochrome P450DM) is the active target site for azole antifungals.Aim and Objective:This study emphasized on evaluation of a series of halogenated imidazole analogues using molecular docking studies for anti-Candidal activity. Furthermore, the model was refined by molecular dynamic simulation.Methods:Halogenated imidazole analogues (PS1-PS30) were obtained from literature for the study. The imidazole analogues were prepared using Chem sketch and mole

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Parmar, Tejasvi H., Chetan B. Sangani, and Mahesh Kulkarni. "Synthesis of novel drug-like small molecules library based on 1." Australian Journal of Chemistry 75, no. 4 (2022): 276–84. http://dx.doi.org/10.1071/ch21238.

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A series of novel ‘drug-like’ small molecules based on 1H-benzo[d]imidazole derivatives bearing furan-2-yl, 4-piperidine and 5-aryl/aminoaryl substitutions were designed and synthesised. The key intermediate tert-butyl-4-(5-bromo-2-(furan-2-yl)-1H-benzo[d]imidazol-1-yl)piperidine-1-carboxylate (5) was synthesised via sequential reaction starting from 4-bromo-1-fluoro-2-nitrobenzene (1). The 5-aryl-substituted molecular library was generated via Suzuki–Miyura coupling of tert-butyl-4-(5-bromo-2-(furan-2-yl)-1H-benzo[d]imidazol-1-yl)piperidine-1-carboxylate (5) with various boronic acids while B

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46

Karun, Sodah, and Khilnani Veena. "DIVERSE SYNTHETIC APPROACHES TO CRAFT IMIDAZOLES - A REVIEW." International Journal of Advanced Research 12, no. 10 (2024): 199–216. http://dx.doi.org/10.21474/ijar01/19633.

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Imidazoles are five membered heterocyclic ring compounds containing two nitrogen atoms as a part of a five membered ring. Imidazole is a pharmacologically important molecule mainly used as antihypertensive, antiplasmodial, antifungal and anticancer agents etc. It can be synthesized by using a variety of starting materials by different synthesis such as â€“ Debus Radziszewski, Van Leusen, Wallach synthesis to name a few. By altering the starting materials different derivatives of imidazole can be synthesized and show a wide range of pharmacological activites. Hence organic chemists are continuo

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Dutta, Satyajit. "Synthesis and anthelmintic activity of some novel 2-substituted-4,5-diphenyl imidazoles." Acta Pharmaceutica 60, no. 2 (2010): 229–35. http://dx.doi.org/10.2478/v10007-010-0011-1.

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Synthesis and anthelmintic activity of some novel 2-substituted-4,5-diphenyl imidazolesA series of 2-substituted-4,5-diphenyl imidazoles1a-jwere synthesized by refluxing benzil with different substituted aldehydes in the presence of ammonium acetate and glacial acetic acid. Structures of the synthesized compounds were confirmed on the basis of IR,1H NMR and mass spectral data. Compounds1a-jwere screened for anthelmintic activity. Test results revealed that compounds showed paralysis time of 0.24 to 1.54 min and death time of 0.39 to 4.40 min while the standard drugs albendazole and piperazine

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Septiana, Ika, Bambang Purwono, Chairil Anwar, Beta Achromi Nurohmah, and Jufrizal Syahri. "Synthesis and Docking Study of 2–Aryl-4,5-diphenyl-1<i>H</i>-imidazole Derivatives as Lead Compounds for Antimalarial Agent." Indonesian Journal of Chemistry 22, no. 1 (2021): 105. http://dx.doi.org/10.22146/ijc.67777.

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Series of 2-aryl-4,5-diphenyl-1H-imidazole derivatives of 2-(4-hydroxy-3-methoxyphenyl)-4,5-diphenyl-1H-imidazole (1), 2-(4,5-dimethoxyphenyl)-4,5-diphenyl-1H-imidazole (2) and 2-(4-methoxyphenyl)-4,5-diphenyl-1H-imidazole (3) were produced and evaluated for their in vitro antimalarial activities against the chloroquine-sensitive Plasmodium falciparum 3D7 strain. A molecular docking study was also carried out against the crystal protein of Plasmodium falciparum dihydrofolate reductase-thymidylate synthase (PfDHFR-TS) (PDB ID: 1J3I.pdb) to predict the interaction between the compounds and prote

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Aggarwal, Mayank, Bhargav Kondeti, Chingkuang Tu, C. Mark Maupin, David N. Silverman, and Robert McKenna. "Structural insight into activity enhancement and inhibition of H64A carbonic anhydrase II by imidazoles." IUCrJ 1, no. 2 (2014): 129–35. http://dx.doi.org/10.1107/s2052252514004096.

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Human carbonic anhydrases (CAs) are zinc metalloenzymes that catalyze the hydration and dehydration of CO2and HCO3−, respectively. The reaction follows a ping-pong mechanism, in which the rate-limiting step is the transfer of a proton from the zinc-bound solvent (OH−/H2O) in/out of the active siteviaHis64, which is widely believed to be the proton-shuttling residue. The decreased catalytic activity (∼20-fold lower with respect to the wild type) of a variant of CA II in which His64 is replaced with Ala (H64A CA II) can be enhanced by exogenous proton donors/acceptors, usually derivatives of imi

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Bagbudar, Zeynep, and Robert Warburton. "Theoretical Studies of Hydrogen Evolution Involving Imidazolium Proton Donors." ECS Meeting Abstracts MA2024-02, no. 61 (2024): 4085. https://doi.org/10.1149/ma2024-02614085mtgabs.

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The hydrogen evolution reaction (HER) is an important electrocatalytic reaction used for the electrochemical production of hydrogen gas. Its reverse reaction, the hydrogen oxidation reaction, is used to produce protons used in electrocatalytic reduction reactions for various electrochemical energy conversion and storage applications. While many fundamental studies have analyzed interfacial reactivity in aqueous HER, analogous mechanistic understanding of HER reactivity in nonaqueous media remains limited. In this presentation, periodic density functional theory (DFT) calculations are applied t

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