1-[1-[2-[(3-Chlorobenzyl)oxy]phenyl]vinyl]-1H-imidazole hydrochloride, a new potent antifungal agent

Ogata, Masaru; Matsumoto, Hiroshi; Hamada, Y.; Takehara, M.; Tawara, Katsuya

doi:10.1021/jm00359a026

Cited by 29 publications

(6 citation statements)

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“…Some other novel antimycotics such as lanoconazole, eberconazole croconazole, and neticonazole are topically applied antimycotics and are imidazole derivatives. All of them display similar activity compared to the other topically applied drugs ( Figure 9 ) [ 146 , 147 , 148 , 149 ].…”

Section: Discussionmentioning

confidence: 89%

Conazoles

Heeres¹,

2010

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This review provides a historical overview of the analog based drug discovery of miconazole and its congeners, and is focused on marketed azole antifungals bearing the generic suffix “conazole”. The antifungal activity of miconazole, one of the first broad-spectrum antimycotic agents has been mainly restricted to topical applications. The attractive in vitro antifungal spectrum was a starting point to design more potent and especially orally active antifungal agents such as ketoconazole, itraconazole, posaconazole, fluconazole and voriconazole. The chemistry, in vitro and in vivo antifungal activity, pharmacology, and clinical applications of these marketed conazoles has been described.

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Section: Discussionmentioning

confidence: 89%

Conazoles

Heeres¹,

2010

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“…These tests were carried out using five fungal species, some of them are pathogenic for human and animals, namely Aspergillus flavus, C. albicans, Chrysosporium tropicum (keratinophyte), Penicillium chrysogenum and Trichophyton rubrum (dermatophyte). All fungal strains were selected based on their pharmacological and clinical relevance as reported previously (Ogata et al, 1983;Fromtling, 1988). All fungal species were cultivated on sabouraud-dextrose agar (Oxoid, England).…”

Section: Microbiology Studymentioning

confidence: 99%

“…It has broad spectrum activity against variety of fungal species in vitro (Fromtling, 1988). It has been proved superior to clotrimazole but less active than miconazole and econazole against C. albicans (Ogata et al, 1983). It is water-insoluble drug, so hydrogel may be an excellent vehicle for the topical delivery of this drug in order to make its release slow from the hydrogel.…”

Section: Introductionmentioning

confidence: 99%

Comparative topical delivery of antifungal drug croconazole using liposome and micro-emulsion-based gel formulations

2013

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“…Econazole Nitrate is a fungistatic antimycotic with a high broad-spectrum synthesized from imidazole, universally used to ight many fungi, especially Candida Albicans (Ogata et al, 1983). Econazole Nitrate is poorly soluble in water (1.48 µg / ml) yet very soluble in methanol (Suñer-Carbó et al, 2017).…”

Section: Introductionmentioning

confidence: 99%

Improvement of econazole nitrate solubility by using surfactants and phospholipids according to optimized experimental design

Bennani¹,

Yachi²,

Alaoui³

et al. 2020

ijrps

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The main purpose of this study is to improve and boost the solubility of Econazole Nitrate in water using phospholipid and surfactants, until it becomes possible to evaluate the utility of a mixture design in order to determine the optimal composition of non-ionic surfactants and phospholipids needed to obtain a significant improvement in the solubility of Econazole Nitrate in water. The design of experiments approach was tested using a mixture design of Lipoïd 75® as phospholipid and Econazole Nitrate, Tween® 80 and Solutol®HS 15 as surfactants,. Solubility was determined by the analysis of samples absorbance at 225 nm. and the measurement size of particles conducted using a Dynamic Light Scattering at the maximum point of solubility. The final results displayed an improvement in solubility with a statistically significant increase in many tested mixtures. Analysis of the design space showed that, the solubility of Econazole Nitrate is importantly affected by the concentration of surfactants. The best obtained test encloses 1% Econazole Nitrate, 2% Tween® 80, 0.5% Lipoid 75®, 2% Solutol®HS 15 and water q. s. for 100% w / w. Our study has demonstrated that optimized experimental design determines the proportions and the effects of every component based on a limited number of experiments.

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1-[1-[2-[(3-Chlorobenzyl)oxy]phenyl]vinyl]-1H-imidazole hydrochloride, a new potent antifungal agent

Abstract: The synthesis and antifungal properties of 1-[1-[2-[(3-chlorobenzyl)oxy]phenyl]vinyl]-1H-imidazole hydrochloride (1 . HCl) are described. Topical application of cream and gel formulation of 1 . HCl showed high efficacy against guinea pig dermatophytosis.

Cited by 29 publications

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Conazoles

Conazoles

Comparative topical delivery of antifungal drug croconazole using liposome and micro-emulsion-based gel formulations

Improvement of econazole nitrate solubility by using surfactants and phospholipids according to optimized experimental design

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