Comparison of the Anti‐inflammatory Activities of Imidazole Antimycotics in Relation to Molecular Structure

Steel, Helen C.; Tintinger, Gregory Ronald

doi:10.1111/j.1747-0285.2008.00694.x

Cited by 41 publications

(22 citation statements)

References 16 publications

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“…Because antifungal drugs are widely used in patients who are immunocompromised to some degree, it is important to determine the possible effects of these therapies on the immune system in vivo [4,11]. Given that little is currently known about the modulating properties of ITC, the aim of the present study was to evaluate the potential immunomodulatory activity of this antifungal drug on the pulmonary levels of 28 molecules with immunological activity in healthy mice.…”

Section: Introductionmentioning

confidence: 99%

Immunomodulatory activity of itraconazole in lung

Naranjo¹,

Henao²,

Zuluaga³

et al. 2017

Trop. J. Pharm Res

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Section: Introductionmentioning

confidence: 99%

Immunomodulatory activity of itraconazole in lung

Naranjo¹,

Henao²,

Zuluaga³

et al. 2017

Trop. J. Pharm Res

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“…[10] Flutrimazole, another imidazole-based wide spectrum antifungal agent, was found to be a good topical anti-inflammatory agent. [11] Therefore, imidazole nucleus seems to be an important pharmacophore for designing new drug candidates [Figure 2].…”

mentioning

confidence: 99%

Synthesis and biological evaluation of di- and tri-substituted imidazoles as safer anti-inflammatory-antifungal agents

et al. 2013

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PURPOSE:In view of the potential pharmacophoric nature of imidazole nucleus, two series of imidazole derivatives, 2,4-disubstituted-1 H-imidazoles (2a-m) and 1,2,4-trisubstituted-1 H-imidazoles (3a-m), were synthesized with an aim of obtaining dual acting compounds i.e., anti-inflammatory and antifungal agents.MATERIALS AND METHODS:The title compounds were synthesized from 4-methoxyphenyl glyoxal (1) following multistep synthesis, and their structures were established on the basis of modern analytical techniques (IR, NMR and MS). The synthesized imidazoles were tested for their in vivo anti-inflammatory activity. In addition to that, some compounds were also evaluated for their analgesic and ulcerogenic effects. The compounds were also evaluated for their in vitro antifungal activity.RESULTS:Di- and tri-substituted imidazole derivatives (2a-m and 3a-m) were successfully synthesized. In in vivo anti-inflammatory test, six compounds (2 h, 2 l, 3 g, 3 h, 3 l and 3 m) exhibited good anti-inflammatory activity (49.58 to 58.02% inhibition) with minimal GI irritation (severity index; 0.17 to 0.34). These compounds were also tested for their analgesic activity and showed appreciable protection (40.53 to 49.60% protection) against saline-induced writhing test. Indomethacin was used as standard drug for comparison. In antifungal test, two compounds (3 h and 3 l) displayed appreciable antifungal activity (MIC; 12.5 μg mL-1) against the fungal strains tested.CONCLUSION:Two compounds, 2-(4-nitrophenyl)-4-(4-methoxyphenyl)-1-phenyl-1H-imidazole (3 h) and 2,4-di-(4-methoxyphenyl)-1-phenyl-1H-imidazole (3 l), emerged as lead compounds having dual biological activities; good anti-inflammatory as well as antifungal effect with lesser GI irritation.

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“…Incubation of human platelet-activating factoractivated neutrophils with various azole antimycotic agents results in statistically significant inhibition of production of leukotriene B4, with itraconazole being the most potent. 28 Additionally, itraconazole has been ability to magnify the anti-inflammatory effect of oral steroids by its inhibition of the hepatic P450 system, thus decreasing clearance of these exogenous steroids. 29 Though the primary mechanism of action of azoles is their antifungal activity, these other secondary mechanisms may further add to the beneficial effects of itraconazole.…”

Section: Discussionmentioning

confidence: 99%