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Some diesters of benzen-1,2-dithiol wit aliphatic and aromatic carboxylic acids were prepared and tested for in vitro antifungal activity. The diacetate and dipropionate of benzen-1,3- and 1,4-dithiol were used as comparison compounds. The substances (Table I; substances I leads to X) were obtained by condensation of benzenedithiols with suitable acylating agents. The fungistatic activity of the products was tested in vitro against the following fungal strains: Candida albicans, Candida tropicalis, Saccharomyces cerevisiae and Trichophyton mentagrophytes. The results show that the diester of benzen-1,2-dithiols with alkanoic acids (Table I) have marked antimycotic activity, much greater than that of clotrimazol. The diaroyl esters of benzen-1,2-dithiol and the diesters of benzen-1,3- and 1,4-dithiols are inactive or only slightly active.

Comparaison des proprietes des composes neutres et ionises de soufre par rapport a l'oxygene

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).

Asymmetric homogeneous hydrogenations of carbon-nitrogen, carbon-oxygen, and carbon-carbon double bonds have been achieved with the same RhI-chiral diphosphine [(–)-diop] catalyst; all the products have the R configuration and a small increase in optical yields is obtained by changing the solvent from methanol to propan-2-ol.

Some diesters of 2-mercaptobenzenmethanthiol and of 2-(2-nitrophenyl)-1,3-benzodithiyne were prepared and tested for in vitro antifungal activity. The substances [Table I: substances (I leads to VIII)] were obtained by condensation of 2-mercaptobenzenmethanthiol with suitable reagents. The antifungal activity of the products was tested in vitro against the following strains: Candida albicans, Saccharomyces cerevisiae and Trichophyton mentagrophytes. It was found that antimycotic activity is shown by only some of the diesters of 2-mercaptobenzenmethanthiol with acyl alkylthiocarbamic groups (Table I). The diesters with aliphatic, aromatic, alkylcarbamic groups and the 2-(2-nitrophenyl)-1,3-benzodithiyne are inactive or only slightly active.

Synthese et reactivite de deux classes d'ions sulfonium: les thiasubstitues et les sels de sulfonium de cycles a trois chainons