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Journal articles on the topic 'Imidazole Compounds'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 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

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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4

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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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

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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7

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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8

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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9

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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10

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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11

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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12

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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13

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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14

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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15

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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16

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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17

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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18

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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19

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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20

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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21

Salam, Shahana, and Rakesh Kumar Jat. "Imidazole Phenanthroline Derivatives: A Promising Application in Modern Medicine." Journal of Drug Delivery and Therapeutics 15, no. 6 (2025): 102–10. https://doi.org/10.22270/jddt.v15i6.7230.

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Purpose: The primary objective of this study is to create a new class of imidazole phenanthroline compounds that target the 1,10-phenanthroline core for its antifungal and antibacterial properties. Methods: Commercially available 1,10-phenanthroline (phen) was nitrated with potassium bromide in the presence of sulfuric and nitric acids to get 1,10-phenanthroline-5,6-dione (phendione), an intermediate molecule, which served as the starting compound for the synthesis of 1H-imidazo [4,5-f] [1,10] phenanthroline compounds. This intermediate product was dissolved in glacial acetic acid and then rea

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22

Al-Soud, Yaseen A., Ala’a H. Al-Ahmad, Luay Abu-Qatouseh, et al. "Nitroimidazoles Part 9. Synthesis, molecular docking, and anticancer evaluations of piperazine-tagged imidazole derivatives." Zeitschrift für Naturforschung B 76, no. 5 (2021): 293–302. http://dx.doi.org/10.1515/znb-2020-0200.

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Abstract New piperazine-tagged imidazole derivatives were synthesized via reaction of 1-alkyl/aryl-5-bromo-2-alkyl-4-nitro-1H-imidazoles 1–3 with piperazine nucleophiles. Nine selected compounds were assessed for their antiproliferative inhibition potency against five human cancer cell lines (MCF-7, PC3, Du145, HepG2 and Dermal/Fibroblast). Compounds 7 and 10 are the most potent anticancer agents on HepG2 cell line with IC50 values of (5.6 ± 0.5 µm) and (29.6 ± 7.6 µm) respectively, and on MCF-7 with IC50 values of (32.1 ± 5.6 µm) and (46.2 ± 8.2 µm) respectively. The molecular docking of comp

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23

Naz, Nimra, Saima Saqib, Rizwan Ashraf, Muhammad Irfan Majeed, and Muhammad Adnan Iqbal. "Synthesis of New Organoselenium Compounds: Characterization and Biological Studies." Macedonian Journal of Chemistry and Chemical Engineering 39, no. 1 (2020): 1. http://dx.doi.org/10.20450/mjcce.2020.1912.

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Two new organoselenium analogs, (3,3'-(1,2-phenylenebis(methylene))bis(2-selenoxo-2,3-dihydro-1H-imidazole-3,1-diyl))bis(methylene) dibenzoate (III) and 3,3'-(1,2-phenylenebis(methylene))bis(1-benzyl-1H-imidazole-2(3H)-selenone) (V), were derived from newly synthesized organic salts 1,1'-(1,2-phenylenebis(methylene))bis(3-(2-phenoxyacetyl)-1H-imidazol-3-ium) chloride (II) and 1,1'-(1,2-phenylenebis(methylene))bis(3-benzyl-1H-imidazol-3-ium) chloride (IV), and each was characterized by various analytical techniques, such as Fourier-Transform Infrared Spectroscopy (FT-IR), UV–visible, and Nuclea

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24

Layla Amer Ibrahim and Radhiyah Abdul Baqi Aldujaili. "Synthesis , Characterization and study the Antimicrobial Activity For Benzo pyran -2-imine and Tetrazole Ring Derivatives." Journal of Kufa for Chemical Sciences 3, no. 3 (2024): 178–200. https://doi.org/10.36329/jkcm/2024/v3.i3.15835.

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The derivatives of [3-(1H-benzo[d]imidazol-2-yl)-2H-chromen-2-imine]L8 and [2-((1H-tetrazol-5-yl)methyl)-1H-benzo[d]imidazole] L7,L9 have been obtained using -(1H-benzo[d]imidazol-2-yl)acetonitrile as starting material .The latter compound was utilized as a key intermediate for the synthesis of new heterocyclic compounds L8,7,9 with good yields. Newly synthesized compounds have been screened for their antimicrobial activity and characterized by analytical and spectral data.

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25

Tarai, Arup, and Jubaraj B. Baruah. "Competing phenol–imidazole and phenol–phenol interactions in the flexible supramolecular environment of N,N′-bis(3-imidazol-1-ylpropyl)naphthalenediimide causing domain expansion." New Journal of Chemistry 41, no. 19 (2017): 10750–60. http://dx.doi.org/10.1039/c7nj02322g.

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Spectroscopic and crystallographic studies on cocrystals of N,N′-bis(3-imidazol-1-yl-propyl)naphthalenediimide (L) with a series of phenolic compounds have revealed that competition to form phenol–imidazole and phenol–phenol synthons causes domain expansion.

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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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27

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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28

Babalola, Benjamin Ayodipupo, and Abayomi Emmanuel Adegboyega. "Computational Discovery of Novel Imidazole Derivatives as Inhibitors of SARS-CoV-2 Main Protease: An Integrated Approach Combining Molecular Dynamics and Binding Affinity Analysis." COVID 4, no. 6 (2024): 672–95. http://dx.doi.org/10.3390/covid4060046.

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One of the most pressing challenges associated with SARS treatment is the emergence of new variants that may be transmissible, causing more severe disease or being resistant to the current standard of treatment. This study aimed to identify potential drug candidates from novel imidazole derivatives against SARS-CoV-2 main protease (Mpro), a crucial drug target for treating viral infection, using a computational approach that integrated molecular docking and dynamics simulation. In this study, we utilized AutoDock Vina within the PyRx workspace for molecular docking analysis to explore the inhi

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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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Shekhovtsov, Nikita A., Elena B. Nikolaenkova, Alexey A. Ryadun, Denis G. Samsonenko, Alexsei Ya Tikhonov, and Mark B. Bushuev. "ESIPT-Capable 4-(2-Hydroxyphenyl)-2-(Pyridin-2-yl)-1H-Imidazoles with Single and Double Proton Transfer: Synthesis, Selective Reduction of the Imidazolic OH Group and Luminescence." Molecules 28, no. 4 (2023): 1793. http://dx.doi.org/10.3390/molecules28041793.

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1H-Imidazole derivatives establish one of the iconic classes of ESIPT-capable compounds (ESIPT = excited state intramolecular proton transfer). This work presents the synthesis of 1-hydroxy-4-(2-hydroxyphenyl)-5-methyl-2-(pyridin-2-yl)-1H-imidazole (LOH,OH) as the first example of ESIPT-capable imidazole derivatives wherein the imidazole moiety simultaneously acts as a proton acceptor and a proton donor. The reaction of LOH,OH with chloroacetone leads to the selective reduction of the imidazolic OH group (whereas the phenolic OH group remains unaffected) and to the isolation of 4-(2-hydroxyphe

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Abu Almaaty, Ali H., Eslam E. M. Toson, El-Sherbiny H. El-Sayed, et al. "5-Aryl-1-Arylideneamino-1H-Imidazole-2(3H)-Thiones: Synthesis and In Vitro Anticancer Evaluation." Molecules 26, no. 6 (2021): 1706. http://dx.doi.org/10.3390/molecules26061706.

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A novel series of N-1 arylidene amino imidazole-2-thiones were synthesized, identified using IR, 1H-NMR, and 13C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative 5 was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles 4d and 5 exhibit pre-G1 apoptosis and cell cycle arrest at G2/M phase. The results of the VEGFR-2 and B-Raf kinase inhibition assay revealed that compounds 4d and 5 di

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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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El Abbouchi, Abdelmoula, Jamal Koubachi, Nabil El Brahmi, and Said El Kazzouli. "Direct arylation and Suzuki-Miyaura coupling of imidazo[1,2-a]pyridines catalyzed by (SIPr)Pd(allyl)Cl complex under microwave-irradiation." Mediterranean Journal of Chemistry 9, no. 5 (2019): 347–54. http://dx.doi.org/10.13171/mjc1911271124sek.

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A short and practical arylation of imidazo[1,2-a]pyridine and imidazole derivatives with aryl halides or aryl boronic acids as coupling partners was successfully carried out using phosphine-free (SIPr)Pd(allyl)Cl as the catalyst [SIPr: (N,N’-bis(2,6-diisopropylphenyl)-4,5-dihydroimidazol-2-ylidene)] ((SIPr)Pd(allyl)Cl complex). 3,6-disubstituted imidazo[1,2-a]pyridine and 5-substituted imidazole compounds were obtained in good to excellent yields in only 1h under microwave-assisted C-H arylation and Suzuki-Miyaura coupling reaction conditions.

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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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Vedekhina, T. S., M. V. Chudinov, and A. Yu Lukin. "Design and synthesis of 4-nitroimidazole derivatives with potential antitubercular activity." Fine Chemical Technologies 18, no. 3 (2023): 219–29. http://dx.doi.org/10.32362/2410-6593-2023-18-3-219-229.

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Objectives. To develop the procedures for synthesis of hybrid molecules with potential anti-tubercular activity containing heterocyclic cores of 4-nitroimidazole and 1,3,4-thiadiazole within the framework of a double-drug strategy and predict bioactivity of target structures and drug-likeness physicochemical parameters.Methods. Target compounds were prepared by classical organic synthesis methods. The structure of the obtained compounds was characterized by melting points, 1H and 13C nuclear magnetic resonance spectroscopy, and high-resolution mass spectrometry. The calculation of the physicoc

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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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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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Qian, Shuai, Patrick Mileski, Adam C. Irvin, Ademola Soyemi, Tibor Szilvási, and Jason E. Bara. "Experimental and Computational Study of the Properties of Imidazole Compounds with Branched and Cycloalkyl Substituents." Liquids 2, no. 1 (2022): 14–25. http://dx.doi.org/10.3390/liquids2010002.

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N-functionalized imidazole compounds with linear alkyl groups have been widely utilized precursors for imidazolium ionic liquids (ILs) while the effects of branched and cycloalkyl substituents on properties of imidazole compounds have not been studied; however, such compounds are just as synthetically accessible as those with linear alkyl groups. In this work, two fundamental properties, density and viscosity, of selected N-functionalized imidazoles bearing iso-propyl, iso-butyl, sec-butyl methylcyclopropyl, cyclopentyl, and methylcyclohexyl groups have been measured in the temperature range o

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Sitapara, S. M., J. H. Pandya, and S. K. Kangad. "Expedited Synthesis and Comprehensive Characterization of Oxomorpholine-Imidazole Derivatives: Unraveling their Remarkable Antimicrobial Activity." Journal of Scientific Research 16, no. 1 (2024): 321–30. http://dx.doi.org/10.3329/jsr.v16i1.67728.

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This research focuses on synthesizing aromatic or heteroaromatic compounds with potential pharmaceutical and medicinal applications. Imidazole derivatives have garnered significant attention due to their versatile therapeutic potential, encompassing a broad spectrum of diseases, including cancer, bacterial infections, fungal infections, and malaria. To accomplish this, we have developed an efficient synthetic route to explore a diverse array of 2-((1,4-diphenyl-1H-imidazol-2-yl)thio)-N-(4-(3-oxomorpholino)phenyl) acetamide derivatives. The structural elucidation of the synthesized compounds wa

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Bhaskar, J. Udaya, G. Srinivasa Rao, Pranab Chatterjee, D. K. Sahoo, S. Srinivasa Rao, and B. Pulla Rao. "Synthesis, Characterization and Antibacterial Screening of Some Novel Compounds containing Multi N-Fused Heterocycles." Asian Journal of Chemistry 36, no. 9 (2024): 2185–90. http://dx.doi.org/10.14233/ajchem.2024.32265.

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An attempt has been made to synthesize novel multi N-fused heterocyclic compounds containing four divergent heterocyclic compounds such as imidazole, pyrimidine, morpholine and indole. A series of N-(4-(1H-benzo[d]imidazol-2-yl)-6-phenylpyrimidin-2-yl)-2-(4-((E)-3-(2-morpholino-9H-pyrido[2,3-b]indol-3-yl)acryloyl)phenylamino)acetamide (6a-c) was accomplished in good yields with 1-(1H-benzo-[d]imidazol-2-yl)ethanone (1) as starting compound and through the formation of (E)-1-(1H-benzo[d]imidazol-2-yl)-3-phenylprop-2-ne-1-ones (2a-c), 4-(1H-benzo[d]imidazol-2-yl)-6-phenylpyrimidin-2-amines (3a-c

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Mendogralo, Elena Y., Larisa Y. Nesterova, Ekaterina R. Nasibullina, et al. "Synthesis, Antimicrobial and Antibiofilm Activities, and Molecular Docking Investigations of 2-(1H-Indol-3-yl)-1H-benzo[d]imidazole Derivatives." Molecules 28, no. 20 (2023): 7095. http://dx.doi.org/10.3390/molecules28207095.

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The treatment of many bacterial and fungal infections remains a problem due to increasing antibiotic resistance and biofilm formation by pathogens. In the present article, a methodology for the chemoselective synthesis of 2-(1H-indol-3-yl)-1H-benzo[d]imidazole derivatives is presented. We report on the antimicrobial activity of synthesized 2-(1H-indol-3-yl)-1H-benzo[d]imidazoles with significant activity against Staphylococcus aureus ATCC 25923, Staphylococcus aureus ATCC 43300 (MRSA), Mycobacterium smegmatis (mc(2)155/ATCC 700084), and Candida albicans ATCC 10231. High activity against staphy

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Singh, Ashok K., Snehlata Katheria, Amrendra Kumar, Asiff Zafri, and Mohd Arshad. "Design, Synthesis, Characterization and Antiproliferative Activities of Ru(II) Complexes of Substituted Benzimidazoles." Asian Journal of Chemistry 31, no. 10 (2019): 2311–18. http://dx.doi.org/10.14233/ajchem.2019.22162.

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Synthesis of [Ru(PPh3)2(BZM)2Cl2] (BZM= LS1, LS2, LS3, LS4 and LS5) where LS1=(1H-benzo[d] imidazole-2-yl)methanethiol, LS2 = 2-(4-bromobutyl)-1H-benzo[d] imidazole, LS3= 2-(4-nitrophenyl)-1H-benzo[d]imidazole, LS4 = 2-(4-chlorophenyl)-1H-benzo[d]imidazole and LS5= 4-(1H-benzo[d]imidazol-2-yl)aniline (BZM = benzimidazoles, PPh3 = triphenylphosphine) and metal complexes as MR, [ Ru (PPh3)4Cl2], MLS1, MLS2, MLS3, MLS4 and MLS5 for use as potential anticancer compounds have been investigated. The complexes have been characterized by elemental analysis, IR, multinuclear NMR, UV-visible and ESI-MS

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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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Li, Sheng-Hui, and Jing Xia. "Design and Synthesis of Crown Ether Functionalized Imidazoles as a New type of Building Blocks." E-Journal of Chemistry 9, no. 4 (2012): 2128–33. http://dx.doi.org/10.1155/2012/818407.

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A simple, convenient and efficient synthesis for a series of crown ether functionalized imidazoles from benzo-15-crown-5 (B15C5), benzo-18-crown-6 (B18C6), imidazole (Im), 2-methylimidazole (mIm), benzimidazole (bIm) and 2-methyl benzimidazole (mbIm) is reported. All these compounds obtained were characterized by IR,1H NMR, ESI-MS and elemental analysis.

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45

Sucipto, Teguh Hari, and Fahimah Martak. "SYNTHESIS OF METAL-ORGANIC (COMPLEXES) COMPOUNDS COPPER(II)-IMIDAZOLE FOR ANTIVIRAL HIV CANDIDATE." Indonesian Journal of Tropical and Infectious Disease 6, no. 1 (2016): 5. http://dx.doi.org/10.20473/ijtid.v6i1.1204.

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The human immunodeficiency virus (HIV) is viruses known as rotaviruses. Potential target for therapeutic is reverse transcriptase (RT), possesses an RNA-dependent DNA polymerase, DNA-dependent DNA polymerase and ribonuclease H fuctions. Imidazoles have high anti-HIV inhibitory activity, some derivates of imidazole reported drugs. 8-chloro-2,3-dihydroimidazole[1,2-b][1,4,2]benzodithiazine-5,5-dioxides and 9-chloro-2,3,4-trihydropyri-mido[1,2-b][1,4,2]benzodithi-azine-6,6-dioxides. This compounds succesfully identified anti-HIV activity. Copper is a bio-essential element and copper complexes hav

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Rufaida, Farheen *. Y. Rajesh Babu 1. "SYNTHESIS AND CHEMICAL CHARACTERIZATION OF BENZIMIDAZOLE FUSED BENZOPYRAN DERIVATIVES AND EVALUATION OF THEIR ANTI-BACTERIAL POTENCY." Journal of Pharma Research 8, no. 3 (2019): 88–93. https://doi.org/10.5281/zenodo.2620330.

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<strong><em>ABSTRACT</em></strong> <strong><em>B</em></strong><em>enz-imidazole fused benzopyran derivatives were prepared by the reaction of 2-(1H-Benzo[d]Imidazol-2-yl)-1phenyl-1H-Benzo[f]chromeno-3-amine with different substituted benzaldehydes. The resulting derivatives were subjected to physical and chemical characterization. The anti-bacterial potency of the synthesized compounds was tested against a set of Gram positive and negative bacteria. The compound 9-(2-methoxyphenyl)-16-phenyl-16H-benzo[4,5]imidazo[1,2-c]benzo[5,6]chromeno[3,2-e]pyrimidine exhibited most potent activity. Detaile

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B., Rajitha* B. Rashmitha S. Ashwini K. Neha N. Prasad M. Ashwini. "An Overview on Synthesis, Properties and Biological Activities of Imidazole and Its Derivatives." International Journal of Pharmaceutical Sciences 3, no. 3 (2025): 2444–53. https://doi.org/10.5281/zenodo.15083575.

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Imidazole belongs to the class of five membered heterocyclic compounds which plays a major role in Medicinal Chemistry. It was synthesized by different methods using different chemicals. This article reviews different methods of synthesis, properties of imidazole, both its natural and synthetic derivatives and pharmacological activities. Imidazole shows wide variety of biological activities such as anti-tubercular activity, anti-inflammatory activity, antimicrobial activity, anthelmintic activity, anti-cancer activity etc., this article reflects on anti-tubercular activity, anti-inflammatory a

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Kürkçüoğlu, Güneş Süheyla, Dursun Karaağaç, and Seray Kekeç. "SYNTHESIS AND SPECTROSCOPIC STUDIES OF COPPER(II)/COBALT(III) CYANIDE COMPOUNDS WITH IMIDAZOLE, 1-METHYLIMIDAZOLE, AND 2-METHYLIMIDAZOLE." Eskişehir Technical University Journal of Science and Technology A - Applied Sciences and Engineering 26, no. 1 (2025): 1–13. https://doi.org/10.18038/estubtda.1541919.

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New Cu(II)/Co(III) cyanide compounds, [Cu3(L)4Co2(CN)12]∙nH2O, with imidazole and methyl derivatives of imidazole have been synthesized in powder form and analyzed using elemental analyses, vibrational (FT-IR and Raman) spectroscopy, and powder X-ray diffraction (PXRD). The elemental analyses of all compounds for C, H, and N were performed and formulas of the compounds were calculated according to the results obtained. In addition, the phase purity of the compounds was confirmed through powder X-ray diffraction (PXRD) analysis. The results of PXRD patterns and vibrational spectroscopic show th

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Cucu (Diaconu), Dumitrela, and Violeta Mangalagiu. "Pyridine-Imidazlolium Salts: Oxidatively Cleavage of N-C Bond via Nitration." Molbank 2019, no. 4 (2019): M1095. http://dx.doi.org/10.3390/m1095.

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Azaheterocycles derivatives with pyridine-imidazole skeleton are compounds of great value for medicinal chemistry. We report herein the nitration of 1,1′-(pyridine-2,6-diylbis(methylene))bis{3-[2-(4-nitrophenyl)-2-oxoethyl]-1H-imidazol-3-ium} bromide using a typical mixture of nitric and sulphuric acid. The nitration occur with the oxidative cleavage of N–C bond between imidazolium ring and methylene group.

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50

Sharma, Pankaj, Chris LaRosa, Janet Antwi, Rajgopal Govindarajan, and Karl A. Werbovetz. "Imidazoles as Potential Anticancer Agents: An Update on Recent Studies." Molecules 26, no. 14 (2021): 4213. http://dx.doi.org/10.3390/molecules26144213.

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Nitrogen-containing heterocyclic rings are common structural components of marketed drugs. Among these heterocycles, imidazole/fused imidazole rings are present in a wide range of bioactive compounds. The unique properties of such structures, including high polarity and the ability to participate in hydrogen bonding and coordination chemistry, allow them to interact with a wide range of biomolecules, and imidazole-/fused imidazole-containing compounds are reported to have a broad spectrum of biological activities. This review summarizes recent reports of imidazole/fused imidazole derivatives a

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