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At least 19 recordsLinked to original sources
PubMed1979

Antifungal activity upon Saccharomyces cerevisiae of iturin A, mycosubtilin, bacillomycin L and of their derivatives; inhibition of this antifungal activity by lipid antagonists.

The antifungal activity of three antibiotics of the iturin group: iturin A, mycosubtilin, bacillomycin L and of eleven methylated and acetylated derivatives of these antibiotics was tested upon Saccharomyces cerevisiae. The lowest MIC values were found for natural antibiotics. The substitution of polar groups diminished the antifungal activity. Various lipids, sterols, fatty acids, fatty acid methyl esters and phospholipids were tested as inhibitors of the antifungal activity of iturin A, mycosubtilin and bacillomycin L. Cholesterol was the strongest inhibitor upon the three antibiotics; ergosterol, oleic acid and cis-vaccenic acid were less potent inhibitors. Among phospholipids, phosphatidyl choline inhibited bacillomycin L and iturin A while diphosphatidyl glycerol inhibited bacillomycin L and mycosubtilin. The inhibitory effect appeared to be dependent on the nature of both the hydrophilic group and the fatty acid part of phospholipids.

Antifungal Agents↗
PubMed1978

A32390A, a new biologically active metabolite. III. In vitro and in vivo antifungal activity.

A32390A, an isonitrile-containing derivative of mannitol, represents a new class of antifungal antibiotics. In vitro antifungal activity of A32390A was found against Candida albicans, Cryptococcus neoformans and Histoplasma capsulatum. In vivo antifungal activity of A32390A was demonstrated in mice infected with C. albicans. Accumulative doses of 37.5 approximately 600 mg/kg, administered subcutaneously over a 24-hour period, showed significant activity without demonstrating toxicity. A32390A was effective, but not as effective as amphotericin B, in reducing the number of Candida cells isolated from the kidney of infected mice. Urinary excretion of A32390A accounted for only 10% of the administered dose. Improved bioavailability of A32390A was accomplished when the antibiotic was combined with polyvinyl pyrrolidone (PVP) in a solid dispersion. Administration of A32390A as a 10% dispersion in PVP resulted in increased urinary excretion of the drug and reduced the amount of drug required for in vivo activity.

Animals↗
PubMedDate not supplied

Chemical structure and antifungal activity of a number of triterpenoids.

Antifungal activity was tested in 49 pentacyclic triterpenoids and their glycosides, of plant and semisynthetic origin. Several of these compounds inhibited the multiplication of the yeast Saccharomyces carlsbergensis. The highest antifungal activity was found in the triterpene glycosides oleanolic acid and hederagenin, which have a free carboxyl group at C 28(27). Triterpenes of the meristotropic acid, macedonic acid, and lupan types had no fungistatic activity at concentrations up to 100 microgram/ml.

Antifungal Agents↗
PubMed1978

[S-Acyl derivatives of thiosalicylamides having antifungal activity. II].

Some S-acyl derivatives of N-alkylthiosalicylamides [Table I: substances (I leads to XXXI)] were prepared and tested for antifungal activity. The substances, most of which had not been previously reported, were prepared by condensation of 2-mercapto-N-alkylbenzamides with suitable acylating agents. The antifungal activity of the compounds was tested in vitro against Candida albicans and Trichophyton mentagrophytes. For some compounds the was tested activity against the above strains fungicidal, Candida tropicalis and Saccharomyces cerevisiae. Many of the compounds proved to have high antifungal activity comparable with that of Clotrimazol. The results extended knowledge on the structure-antifungal activity relationships of this class of compounds. The compounds with the highest antifungal activity were: 2-acetylmercapto-N,n-heptylbenzamide (XXVIII); 2-acetylmercapto-5-Cl-N,n-propylbenzamide (XIV); 2-acetylmercapto-N,n-octylbenzamide (XXXI); 2-acetylmercapto-N,n-pentylbenzamide (XXV); 2-acetylmercapto-N,n-hexylbenzamide (XXVII).

Antifungal Agents↗
PubMed1978

Semisynthetic cephalosporins with antifungal activity: laboratory studies on 2-pyridinethiol 1-oxide cephalosporins.

Cephalosporins are chemotherapeutic agents whose spectrum and use are limited to antibacterial activity. Therefore, it was of interest to find several new semisynthetic cephalosporins which possess in vitro antifungal activity against Trichophyton mentagrophytes, Candida albicans and certain other yeasts. Five new cephalosporins containing the 2-pyridinethiol 1-oxide grouping were examined. Four with this heterocyclic moiety in the 3-position were found to have activity. One with the grouping in the 7-acyl-side chain was inactive. The degree of the antifungal activity was influenced by the substituent at the 7-position. The cephalosporin with a p-hydroxyphenylglycyl side chain was the most potent against the fungal strains studied. Despite this in vitro antifungal activity, none of the compounds protected mice against a systemic Candida albicans infection. All of these cephalosporins had broad spectrum in vitro and in vivo antibacterial activity.

Animals↗
PubMed1979

[Preparation and antifungal activity of carbamic and thiocarbamic esters of thiophenols].

A series of N-substituted carbamic and thiocarbamic esters of thiophenols [substances (I leads to XLII)] was prepared and tested for in vitro antifungal activity. The substances were obtained by condensation of thiophenols with suitable isocyanates and isothiocyanates. The antifungal activity of the products was tested in vitro against the following strains: Candida albicans, Candida tropicalis, Saccharomyces cerevisiae and Trichophyton mentagrophytes. The results obtained, given in the Table I, show that the carbamic and thiocarbamic esters of the thiophenols examined have marked antifungal activity. The results give some information on structure-activity relationships and also show that in general the derivatives of dithiocarbamic acid are more active than the bioisosteric derivatives of thiocarbamic acid. Of the compounds examined the most active were esters of N-benzyl and N-allyldithiocarbamic acid.

Antifungal Agents↗
PubMed1976

Effect of culture media on the antifungal activity of miconazole and amphotericin B methyl ester.

The capacity of four culture media to obfuscate the antifungal activity of miconazole and amphotericin B methyl ester was evaluated qualitatively by examination of five isolates each of Candida albicans, Candida tropicalis, Candida parapsilosis, Torulopsis glabrata, and Cryptococcus neoformans, and quantitatively by determination of the absolute minimal inhibitory concentrations for a strain of C. albicans. Miconazole, like the predecessor imidazole (clotrimazole), was antagonized by two complex, undefined media (Sabouraud's glucose and brain-heart infusion agars) but not by either of two synthetic formulations (synthetic amino acid medium, fungal and modified yeast-nitrogen base). The antifungal activity of amphotericin B methyl ester, like that of the parent compound amphotericin B, was not materially affected by the culture medium used for testing. When added separately to synthetic amino acid medium (fungal), neither purines nor pyrimidines antagonized miconazole. Ether extraction of Sabouraud's glucose agar failed to diminish the antagonism of this medium for miconazole.

Amphotericin B↗
PubMed1978

[S-acylderivatives of thiosalicylamides with antifungal activity. I].

A series of S-acylderivatives of N-ethylthiosalicylamide (substances I leads to XXIII) was prepared and tested for in vitro antifungal activity. The substances, not previously reported, were prepared by the reaction of 2-mercapto-N-ethylbenzamide with suitable acylating agents. The fungistatic activity of the prepared products was tested in vitro against Candida albicans and Trichophyton mentagrophytes. The results given in Table I show that the S-acylderivatives of N-ethylthiosalicylamides have interesting antifungal activity. From examination of the results (Tables I and II) some information on the structure-activity relationship was obtained. 2-Acetylmercapto-N-ethylbenzamide (I) and 2-propionylmercapto-N-ethylbenzamide (III) proved the most active of the compounds tested.

Antifungal Agents↗
PubMed1979

Antibacterial and antifungal activities of isatin N-Mannich bases.

The antimicrobial and antifungal activities of 29 congeneric isatin N-Mannich bases were investigated by testing against standard test microorganisms and 21 pathogenic Gram-negative microorganisms. Considerable growth inhibition of Gram-negative bacteria and yeasts and slight inhibition of Gram-positive bacteria resulted when they were treated with the various N-Mannich bases of isatin and 5-nitroisatin, respectively.

Anti-Bacterial Agents↗
PubMed1976

Studies on the biological effects of deuteriated organic compounds. III. Antifungal activity of perdeuteriated fatty acids on dermatophytes in vivo experimental microsporie in guinea pigs.

Investigations on the antimycotic properties of perdeuteriated fatty acids were carried out on Microsporum cains infections in vivo. The study was performed on experimental microsporie in guinea pigs using four different methods, all based on the ability of M. canis to cause alopecia. Perdeuteriated n-hendecanoic acid showed in vivo a statistically significant enhanced antimycotic effect compared to its unlabelled analogue. This is in accordance with our previous observations in vitro conditions. The remaining perdeuteriated fatty acids (C12--C18) showed no statistically significant growth retarding effect on M. canis infections in guinea pigs when compared with their unlabelled analogues. The present study attempts to ascertain if some perdeuteriated fatty acids have any antifungal activity in vivo conditions. Our previous papers (3,4) concerning the evaluation of the antifungal activity of some perdeuteriated fatty acids on dermatophytes in vitro, demonstrated that the perdeuteriation of n-hendecanoic acid, lead to a pronounced antimycotic effect on common dermatophytes as e.g. E. floccosum, T. rubrum, M. canis and T. mentagrophytes. As our previous results indicate a decreasing of fungistasis with an increasing carbon-chain length of the perdeuteriated fatty acids, we have attempted to verify this observation in vivo conditions. A special interest was, of course, focused on the most promising compound, the perdeuteriated n-hendecanoic acid.

Alopecia↗
PubMed1976

Studies on the biological effects of deuteriated organic compounds. I. Antifungal activity of perdeuteriated fatty acids on dermatophytes in vitro.

The antifugal activity of some perdeuteriated fatty acids, with normal chain 11 to 18 carbon atoms, was investigated on common dermatophytes Epidermophyton floccosum, Microsporum canis, Trichophyton mentagrophytes and T. rubrum under in vitro conditions. These studies were performed by dilution technique and with respiratory measurements, Perdeuteriation of some fatty acids increases their inhibitory effect on the dermatophyte growth. Perdeuteriated n-hendecanoic acid proved to be the most active of the substances tested. Possible mechanisms behind the enhanced antifungal activity due to the perdeuteriation of fatty acids are discussed.

Antifungal Agents↗
PubMed1977

Antifungal activity of four tetracycline analogues against Candida albicans in vitro: potentiation by amphotericin B.

The antifungal activities of four tetracycline analogues in combination with amphotericin B (AmB) were determined against 20 strains of Candida albicans. When a microtiter checkerboard technique was used, minocycline (less than or equal to 10 microgram/ml) acted synergistically with AmB against all strains, whereas doxycycline had a reduced effect, and demeclocycline and tetracycline had no potentiating effect at this concentration. Killing-curve experiments with two strains of C. albicans demonstrated that the combination of minocycline and AmB produced a decrease in number of colony-forming units (cfu) of greater than 2 logs in 4 hr and a 4-log decrease in cfu in 24 hr at concentrations (minocycline, 0.64 microgram/ml; AmB, 0.1 microgram/ml) that were subinhibitory when each agent was used alone and that are readily achieved in human serum and body fluids with conventional doses. The killing-curve technique indicated that doxycycline had an intermediate degree of synergistic activity, whereas tetracycline had no synergistic activity at clinically relevant concentrations.

Amphotericin B↗
PubMed1976

Antifungal activity of 4-substituted crotonic acid esters.

Twenty-three 4-substituted crotonic acid esters were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes. For the analogues of the methyl ester containing substituents in the 4 position, the following order of fungitoxicity was observed: I greater than Br greater than Cl greater than CH3S greater than CH3O greater than F=H. Of the homologues of the esters of the 4-iodo and 4-bromo compounds which included methyl, ethyl, n-propyl, n-butyl, n-pentyl, and n-hexyl, ethyl 4-iodocrotonate was most toxic to the four fungi at pH 7.0 in the presence of 10% beef serum (C. albicans, 18mug/ml, A. niger, 40 mug/ml, M. mucedo, 5 mug/ml, T. mentagrophytes, 4 mug/ml). It is believed that the mechanism of fungitoxicity is due, in part, to a nucleophilic reaction involving SH-containing compounds. This is based on the correlation of fungitoxicity with the order of leaving groups in the nucleophilic reaction and the protection against the toxicity of the test compounds to the fungi by cysteine and glutathione.

Antifungal Agents↗
PubMed1979

[S-Acyl derivatives of thiosalicylamides with antifungal activity. III].

Some S-acylderivatives of N-monosubstituted amides of thiosalicylic acid in which the N substituents were unsaturated alkyl groups, cyclic or branched saturated alkyl groups, aromatic or aralkyl groups, were prepared and tested for antifungal activity. The substances which were all new were prepared by condensation of 2-mercapto-N-alkylbenzamides with suitable acylating agents. The fungistatic activity of the products was tested in vitro against the following: Candida albicans and Trichophyton mentagrophytes. The results reported in Table I underline the importance of the S-acylderivatives of N-monosubstituted amides of thiosalicylic acid as antifungal agents. Study of the results in Table I has also given some insight on the structure-activity relationships. The S-acyl-N-aralkylthiosalicylamides proved the most active of the compounds tested.

Antifungal Agents↗