Imidazole Derivatives as Potential Therapeutic Agents

Sharma, Archana; Kumar, Vipin; Kharb, Rajeev; Kumar, Sunil; Sharma, Prabodh Chander; Pathak, Dharam Pal

doi:10.2174/1381612822666160226144333

Cited by 39 publications

(21 citation statements)

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“…Imidazoles and nitroimidazoles belong to a group of heterocyclic and nitroheterocyclic compounds that are mainly used as broad-spectrum anti-infectious agents. 1 Adverse effects are relatively rare 2 ; in particular, allergic contact dermatitis (ACD) is comparatively rare, considering the high prescription rates. 3 In a few cases of ACD caused by metronidazole 4,5 and clotrimazole, 6 , sensitivity to methylchloroisothiazolinone (MCI)/methylisothiazolinone (MI) coexisted.…”

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confidence: 99%

Sensitivity to imidazoles/nitroimidazoles in subjects sensitized to methylchloroisothiazolinone/methylisothiazolinone: A simple coincidence?

et al. 2018

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Imidazoles and nitroimidazoles belong to a group of heterocyclic and nitroheterocyclic compounds that are mainly used as broad-spectrum anti-infectious agents. 1 Adverse effects are relatively rare 2 ; in particular, allergic contact dermatitis (ACD) is comparatively rare, considering the high prescription rates. 3 In a few cases of ACD caused by metronidazole 4,5 and clotrimazole, 6 , sensitivity to methylchloroisothiazolinone (MCI)/methylisothiazolinone (MI) coexisted. MATERIALS AND METHODS BetweenJune 2015 and December 2016, 149 patients (35 men and 114 women; mean age 40.0 years) recently diagnosed as being sensitized to MCI/MI (0.02% aq.), mainly because of the use of cosmetics, were patch tested with phenethyl imidazoles (econazole nitrate, fenticonazole nitrate, isoconazole nitrate, ketoconazole, miconazole nitrate, sertaconazole nitrate, and tioconazole) and phenmethyl imidazoles (bifonazole nitrate and clotrimazole), all at 2% pet., 7 as well as with nitroimidazoles, both antiprotozoals (metronidazole and tinidazole) and antihelmintics (albendazole and mebendazole), all at 5% pet. (FIRMA, Florence, Italy). We also tested MCI MI at the same concentrations as in the commercial blend (0.015% aq. and 0.005% aq., respectively); MI 0.2% aq. was also tested to avoid false-negative reactions. 8 Patch tests were performed in accordance with ESCD recommendations, with Haye's Test Chambers (Haye's Service, Alphen aan den Rijn, The Netherlands) on Soffix tape (Artsana, Grandate, Italy). Micropipettes were used for aqueous allergens, and haptens were simultaneously occluded for 2 days. Readings were performed on day (D) 2 and D4. A computerized conformational analysis (TRYDENT V1.0.0 software; Molecular Modeling for Medicinal Chemists, Wavefunction, Irvine,California) was carried out to study the spatial electron cloud geometries of MCI, MI and the imidazoles/nitroimidazoles that gave positive reactions in patch tests. 9

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confidence: 99%

Sensitivity to imidazoles/nitroimidazoles in subjects sensitized to methylchloroisothiazolinone/methylisothiazolinone: A simple coincidence?

et al. 2018

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“…The good performance of surface extract in anti-settlement assay might be due to the presence of a large num- Gadhi, El-Sherbiny, Al-Sofyani, Ba-Akdah, Satheesh ber of compounds, which need further studies. Some of the compounds identified from the surface extract such as azetidine-2-one, piperidine, propanamide and imidazole derivatives have potent pharmacological activities (Olgen et al 2008;Noolvi et al 2014;Sharma et al 2016;Zhang et al 2017). Imidazole and piperidines exhibited antifouling activities in previous studies (Majik et al 2014;Huang et al 2014).…”

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confidence: 99%

Antimicrofouling activities of marine macroalga Dictyota dichotoma from the Red Sea

Gadhi

El‐Sherbiny

Al-Sofynai

et al. 2019

Jour. Agri. & Mar. Scie.

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Introduction. Marine organisms produce a variety of secondary metabolites mainly for achieving the defence against the competitors and predators. These compounds could be used as natural product antifoulants for the management of biofouling growth on marine structures. Objectives. To understand the antifouling defence strategies of marine macroalgae collected from the Red Sea. Methodology. The macroalga Dictyota dichotoma was collected from the Obhur Creek of Red Sea, Saudi Arabia and extracted using methanol. Surface and total extraction methods were performed and tested against a bacterial strain isolated from the microfouling assemblage. Results. The extracts obtained from the macroalgal samples have strong antibacterial and antibiofilm activities against the bacterial strain isolated from the marine microfouling assemblage. The total extracts showed strong bacterial growth inhibitory activities in culture plate method. In microtitre plate assay, surface extract showed strong biofilm inhibitory activity. GC-MS analysis indicated considerable variations in the metabolic profile of the surface and total extracts. Conclusion. This study revealed the importance of surface-associated compounds in antifouling defence mechanism of the marine macroalgae.

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“…In recent years, imidazole-associated natural products have gained significant scientific exploration for possible antiparasitic drug development [14]. The imidazole nucleus represents an important heterocyclic core in several biologically active compounds [15,16] and has been found to exhibit unique medicinal properties such as; excellent tissue penetrability and permeability, high bioavailability and low incidence of adverse toxicity [17].…”

Section: Introductionmentioning

confidence: 99%

Paenidigyamycin G: 1-Acetyl-2,4-dimethyl-3-phenethyl-1H-imidazol-3-ium

Tetevi

Kwain

Mensah

et al. 2019

Molbank

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The Ghanaian Paenibacillus sp. DE2SH (GenBank Accession Number: MH091697) is a prolific producer of potent antiparasitic alkaloids. Further detailed study of the culture broth of this strain produced the compound Paenidigyamycin G (1), which is a derivative of the known antiparasitic compound Paenidigyamycin A (2). Compound (1) was isolated on HPLC at tR ≈ 37.5 min and its structure determined by IR, UV, MS, 1D, and 2D-NMR data. Compound 1 produced weak to moderate antileishmanial and antitrypanosomal activity when tested against Leishmania donovani (Laveran and Mesnil) Ross (D10) and Trypanosoma brucei subsp. brucei strain GUTat 3.1 with IC50 = 115.41 and 28.75 μM, respectively. This result is interesting since the parent compound 2 is known to possess consistent and potent antiparasitic activity. However, 1 displayed a promising selectivity profile towards T. brucei subsp. brucei due to its relatively low toxicity against normal mouse macrophages RAW 264.7 cells (SI = 8.70). Given that compound 1 is also the main metabolite found in the hexane fraction of all extracts produced by Paenibacillus sp. DE2SH when it is co-cultured with other bacteria strains, it must possess some unique biological functions which should make it an excellent candidate for further biological activity screening in other bioassays.

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Imidazole Derivatives as Potential Therapeutic Agents

Abstract: It is anticipated that the information compiled in this paper will be useful and motivating to prospective researchers working on this heterocylic scaffold.

Cited by 39 publications

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Sensitivity to imidazoles/nitroimidazoles in subjects sensitized to methylchloroisothiazolinone/methylisothiazolinone: A simple coincidence?

Sensitivity to imidazoles/nitroimidazoles in subjects sensitized to methylchloroisothiazolinone/methylisothiazolinone: A simple coincidence?

Antimicrofouling activities of marine macroalga Dictyota dichotoma from the Red Sea

Paenidigyamycin G: 1-Acetyl-2,4-dimethyl-3-phenethyl-1H-imidazol-3-ium

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