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Biomedical subjects

M Veronese

Publications and source records attributed to M Veronese.

At least 37 records · Page 2Linked to original sources

Synthesis and antimycotic activity of alpha-aryl-beta,N-imidazolylalkyl benzyl ethers.

A new series of alpha-aryl-beta,N-imidazolylalkyl benzyl ethers was synthesized and tested for antimycotic and antimicrobial activity. Most of the compounds was highly active in vitro against fungi and gram-positive bacteria. The alpha,4-phenylthiophenyl-beta,N-imidazolylethyl benzyl ether (7) and the alpha,4-biphenyl-beta,N-imidazolylethyl benzyl ether (17) showed higher antifungal activity than 1-[2,4,dichloro-beta-(2,4-dichlorobenzyloxy)phenethyl]imidazole (miconazole) against Candida albicans. None of the compounds was more active than miconazole against Trichophyton mentagrophytes. The most interesting compounds of the series were assayed in vivo, but their activity was inconstant and always lower than that of miconazole.

Animals↗

The Salmonella mutagenicity assay on fenticonazole, a new antifungal imidazole derivative.

alpha-(2,4-Dichlorophenyl)-beta,N-imidazolylethyl 4-phenylthiobenzyl ether nitrate (fenticonazole, Rec 15/1476), a new potent antibacterial and antifungal imidazole derivative, was tested for mutagenicity in the Salmonella reversion assay developed by Ames et al. Fenticonazole was found to be negative for strains TA 1535, TA 1537, TA 1538, TA 98, TA 100 with and without microsomal activation.

Animals↗

New alpha-aryl-beta,N-imidzolylethyl benzyl and naphthylmethyl ethers with antimycotic and antibacterial activity.

A new series of alpha-aryl-beta,N-imidazolylethyl benzyl and naphthylmethyl ethers was synthesized and tested for antimycotic and antimicrobial activity. All compounds showed antifungal activity; most of them were also active against gram-positive bacteria, whereas no activity was detected against gram-negative bacteria. Structure-activity relationships are discussed. The alpha-(2,4-dichlorophenyl)-beta,N-imidazolylethyl 4-phenylthiobenzyl ether nitrate (8), which showed good skin tolerability and in vivo antimycotic activity comparable with or better than 1-[2,4-dichloro-beta-(2,4-dichlorobenzyloxy)phenethyl]imidazole (miconazole) and 1-(alpha-(o-chlorophenyl)benzhydryl]imidazole (clotrimazole), was selected for further researches.

Animals↗

Fenticonazole, a new imidazole derivative with antibacterial and antifungal activity. In vitro study.

The activity of alpha-(2,4-dichlorophenyl)-beta,N-imidazolylethyl 4-phenylthiobenzyl ether nitrate (fenticonazole, Rec 15/1476) compared with those of reference drugs, was tested in vitro on various bacteria and fungi. This compound showed in vitro an excellent activity against gram-positive microorganisms. The antifungal activity spectrum is very broad: dermatophytes, yeasts and dimorphic fungi were the most susceptible organisms. Fenticonazole showed in vitro at pH range 4-5 the highest activity against yeasts. The addition of inactivated bovine serum to the culture medium led to a slight decrease in activity of all the tested substances.

Anti-Bacterial Agents↗

Antifungal activity of fenticonazole in experimental dermatomycosis and candidiasis.

The antifungal activity of alpha-(2,4-dichlorophenyl)-beta,N-imidazolylethyl 4-phenylthiobenzyl ether nitrate (fenticonazole, Rec 15/1476) in experimental dermatomycosis and candidiasis in guinea pigs was studied. Fenticonazole proved to be a very active drug with a healing capacity generally higher than that of the reference compounds. The adequate range of activity was from 1% to 3%, giving complete healing without relapses in 100% of cases treated. Fenticonazole is presently undergoing further experimental studies and on the basis of our results a clinical trial would therefore seem to be essential.

Animals↗

Mutagenicity studies on fenticonazole, a new antifungal imidazole derivative.

The forward mutational assay on Schizosaccharomyces pombe and the mitotic gene conversion assay on Saccharomyces cerevisiae were performed in order to verify whether alpha-(2,4-dichlorophenyl)-beta,N-imidazolylethyl 4-phenylthiobenzyl ether nitrate (fenticonazole, Rec 15/1476) shows a potential mutagenicity. In both tests the drug does not seem to possess any mutagenic activity when compared with mutagenic standards.

Animals↗

Antimicrobial activity of tibezonium (TBZ).

The activity in vitro of tibezonium (Rec 15-0691), a new 1,5-benzodiazepine derivative, has been investigated. The drug was found active especially against Streptococcus, Diplococcus and Corynebacterium strains which are agents of oropharyngeal diseases. The activity of tibezonium was pH dependent against Staphylococcus aureus SG 511 and Streptococcus pyogenes 821 (at pH 8.0-8.5 It was more active) and the presence of horse serum provoked a small decrease of the antimicrobial properties. No interference on the activity of the tibezonium has been found in presence of smokers and non-smokers saliva.

Anti-Bacterial Agents↗