Comparison of In Vitro Activity of Undecylenic Acid and Tolnaftate against Athlete’s Foot Fungi

Amsel, Lewis P.; Cravitz, Leo; Vanderwyk, Raymond; Zahry, Safwat

doi:10.1002/jps.2600680338

Cited by 9 publications

(6 citation statements)

References 5 publications

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“…Although the excellent antidermatophytic activity of tolnaftate in vitro and in vivo as well as in clinics has already been reported (1,4,8,12,14,17), in this study piritetrate was found to be more active than tolnaftate in vitro and in vivo, primarily against dermatophytes, irrespective of the tested genera and strains. Furthermore, piritetrate exhibited considerable in vitro activity against other groups of fungi, such as dematiaceous fungi, dimorphic fungi, and some other filamentous fungi, showing some difference among strains, whereas almost all the test species and strains of these groups were much less susceptible to tolnaftate.…”

Section: Discussionmentioning

confidence: 42%

“…The yeast fungi were not susceptible to either compound, with the exception of a few strains of Cryptococcus neoformans which were considerably susceptible to piritetrate. Such (1,5,7,17,19). Variation of incubation time, inoculum size, and medium pH within a limited range did not significantly affect the antidermatophytic activity of piritetrate or tolnaftate.…”

Section: Discussionmentioning

confidence: 99%

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In vitro and in vivo activities of piritetrate (M-732), a new antidermatophytic thiocarbamate

Iwata

Yamashita

Uehara

1989

Antimicrob Agents Chemother

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Piritetrate (M-732), a new topical antifungal agent belonging chemically to the thiocarbamates, was demonstrated to possess a potent selective antidermatophytic activity. In terms of its MICs in susceptibility testing, mainly done by using Sabouraud dextrose agar plates, piritetrate exhibited several-to 10-fold-stronger antidermatophytic activity than tolnaftate, a reference thiocarbamate. Furthermore, piritetrate was found to show a broader antifungal spectrum than tolnaftate; relatively many species and strains of dematiaceous fungi, dimorphic fungi, and some other Mifamentous fungi as weUl as a few strains of Cryptococcus neoformans were fairly susceptible to piritetrate, while almost all the tested species and strains were resistant to tolnaftate. All the tested species of the genus Candida were, however, resistant to both compounds. Variables which can influence antimicrobial activity caused few changes in the MICs of either compound against Trichophyton mentagrophytes; however, an increase in the inoculum size resulted in a significant increase in the MICs. The antidermatophytic activities of piritetrate and tolnaftate were fungistatic but not fungicidal. Piritetrate also exhibited a more potent in vitro anti-T. mentagrophytes activity than clotrimazole or tolciclate. Piritetrate and tolnaftate had no antibacterial activity. The in vivo activity of topically administered piritetrate against experimental dermal infection of guinea pigs with T. mentagrophytes was more effective than that of tolnaftate both mycologically and clinically. Piritetrate manifested no acute toxicity in laboratory animals when administered even in large quantities by the oral, intraperitoneal, and topical routes.Piritetrate (M-732) is a new thiocarbamate compound [methyl(6-methoxy-2-pyridyl)carbamothioic acid 0-5,6,7,8-tetrahydro-2-naphthalenyl ester (C18H20N202S)] which was synthesized by the Chemical Research Laboratory, Tosoh Corporation (formerly, Toyo Soda Manufacturing Co., Ltd.), Yamaguchi-ken, Japan. The structure of piritetrate is shown in Fig. 1 MATERIALS AND METHODSAntifungal agents. Piritetrate, tolnaftate, and tolciclate were provided by Tosoh Corporation. Clotrimazole was a gift from Bayer Yakuhin Co., Ltd., Tokyo, Japan. For in vitro antifungal and antibacterial tests, stock solutions at a concentration of 10 mg/ml were prepared by dissolving the compounds in dimethyl sulfoxide, which proved to be stable for many months when stored at 4°C in the dark. For in vivo antifungal tests, piritetrate and tolnaftate were formulated as 1 and 2% creams suspended in a mixture of polyethylene glycol 400 and 1540 (6:4 [vol/vol]) and were administered topically. Piritetrate was also tested for acute toxicity, the method for which will be described later.Organisms Table 1). The recent isolates of dermatophytes, generously provided by S. Kagawa, Department of Dermatology, Tokyo Medical and Dental University, Tokyo, Japan (see Table 2), were compared with the stock cultures of dermatophytes for susceptibility to piritetrate and the t...

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Section: Discussionmentioning

confidence: 42%

Section: Discussionmentioning

confidence: 99%

In vitro and in vivo activities of piritetrate (M-732), a new antidermatophytic thiocarbamate

Iwata

Yamashita

Uehara

1989

Antimicrob Agents Chemother

View full text Add to dashboard Cite

show abstract

“…We also wish to present in vitro and in uivo data using standard methods, which show, in contrast to the Amsel et al (1) report, that tolnaftate is superior to the undecylenates. These conclusions were based on the methods, materials, and results of experiments presented in their paper.…”

mentioning

confidence: 97%

“…Our criticisms of the Amsel et al (1) report are as follows: 1. Standard procedures for determination of the minimum fungicidal concentration in broth or agar were not used.…”

mentioning

confidence: 98%

“…Amsel et al (1) compared the in uitro antifungal activity of undecylenic acid and tolnaftate and drew several conclusions. Among these conclusions were: ( a ) the undecylenate product killed the test organisms more rapidly than the tolnaftate-containing product; (b) undecylenates possibly are more effective in in uitro killing time than tolnaftate alone, and this finding probably applies to the commercial powders; and (c) although the concentrations Values between tolnaftate and undecylenates were statistically significant (p < 0.OOOl) at each time point.…”

mentioning

confidence: 99%

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Comparative in vitro and in vivo antifungal activity of tolnaftate and various undecylenates

Loebenberg¹,

Parmegiani²,

Hanks³

et al. 1980

Journal of Pharmaceutical Sciences

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Comparison of In Vitro Activity of Undecylenic Acid and Tolnaftate against Athlete’s Foot Fungi

Cited by 9 publications

References 5 publications

In vitro and in vivo activities of piritetrate (M-732), a new antidermatophytic thiocarbamate

In vitro and in vivo activities of piritetrate (M-732), a new antidermatophytic thiocarbamate

Comparative in vitro and in vivo antifungal activity of tolnaftate and various undecylenates

Comparative in vitro and in vivo antifungal activity of tolnaftate and various undecylenates: A rebuttal

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