Biomedical subjects

T Modena

Publications and source records attributed to T Modena.

27 records · Page 2Linked to original sources

PubMed1980

[Thiocarbamic and carbamic esters of benzenedithiols with antimycotic activity].

o-, m- and p-phenylen esters of some dithio and thiol carbamic acids N-monosubstituted were prepared and tested for in vitro antifungal activity. The substances studied [Tables I leads to III; substances (I leads to XXI) were all new and were prepared by the reaction of benzenethiols with suitable isothiocyanates or isocyanates. The fungistatic activity of the products was tested in vitro against the four following strains: Candida albicans, Candida tropicalis, Saccharomyces cerevisiae and Trichophyton mentagrophytes. The results show that the diesters of N-monosubstituted carbamic acids of benzen-1,2-dithhiol (Table I) have marked antimycotic activity, of the same order or greater than that of clotrimazol. Among the thiocarbamic and carbamic diesters of benzen-1,3- and 1,4-dithiol, the most active are the N-benzyl- and N-beta-phenyethyldithiocarbamic derivatives.

Antifungal Agents↗

PubMed1980

[The antimycotic activity of acyl derivaties of 2-oximino-1,3-benzodithiol].

A series of esters of 2-oximino-1,3-benzodithiol [substances (II leads to XV)] was prepared and tested for antifungal activity in vitro. The substances were obtained by condensation of 2-oximino-1,3-benzodithiol with suitable acylation agents. The fungistatic activity of the products was tested in vitro against the four strains: Candida albicans, Candida tropicalis, Saccharomyces cerevisiae and Trichophyton mentagrophytes. The results reported in the Table I show the interesting antimycotic activity observed for 2-oximino-1,3-benzodithiol, which is apparently connected with the presence of a free oximino group.

Antifungal Agents↗

PubMed1979

[S-acyl derivatives of thiosalicylamides and their anti-fungal activity. IV].

Some S-acyl derivatives of N-alkylthiosalicylamides [Table I, II: substances (I leads to XXXIII)] in which the acyl group on S in a carbamic or thiocarbamic N-monosubstituted group were prepared and tested in vitro for antifungal activity. All the substances which are not previously recorded were prepared by condensation of 2-mercapto-N-alkylbenzamides with suitable isocyanates or isothiocyanates. The fungistatic activity of the products prepared was tested in vitro against the two strains: Candida albicans and Trichophyton mentagrophytes. The results (Table I and II) show that the N-monosubstituted S-carbamoyl and S-thiocarbamoyl derivatives of N-monosubstituted amides of thiosalicyclic acid have marked in vitro antimycotic activity. Many derivatives have activity of the same order of magnitude as that of clotrimazole and of these the most active compound is 2-(N-phenylcarbamoylmercapto)-N,n-heptylbenzamide (XXVI).

Antifungal Agents↗

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↗

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↗

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↗

PubMedDate not supplied

Evaluation of enzyme stability during preparation of polylactide-co-glycolide microspheres.

This work was aimed at studying enzyme prolidase stability and its interactions with the reagents and the process conditions involved in preparation, by an emulsification process, of prolidase loaded poly(lactide-co-glycolide) (PLGA) microparticulate systems. Enzyme stability was tested with respect to contact with methylene chloride, ethyl acetate, PLGA polymers, and several agents used as emulsifiers such as polyvinyl alcohol (PVA), polyvinyl pyrolidone (PVP), carboxymethyl cellulose (CMC) and sodium oleate (NaOl). Enzyme stability to temperature and mechanical stirring was also evaluated. Prolidase-loaded PLGA microspheres were prepared and evaluated in terms of protein activity. The results obtained showed that the prolidase-loaded PLGA microspheres can be prepared only upon enzyme stabilization by addition of both BSA and MnCl(2) into its TRIS solution. Methylene chloride was the suitable organic solvent to be used in the double emulsion process, together with PVA as dispersing agent in the outer aqueous phase. Low temperatures during the emulsification step and very short process times are recommended, in order to maintain enzyme activity at its maximum. In these conditions spherical microspheres were obtained, releasing active prolidase for up to 15 days.

Animals↗

PubMedDate not supplied

Evaluation of process parameters involved in chitosan microsphere preparation by the o/w/o multiple emulsion method.

Chitosans are interesting biopolymers largely studied for applications in the medical and pharmaceutical fields. In this work, an o/w/o multiple emulsion technique was used for the preparation of hydrophobic drug loaded microspheres. Moreover, the influence of critical variables (concentration of acetic acid in the polymer solution and drug-polymer ratio) on microsphere morphology and drug content was evaluated. Two chitosans of different molecular weights and deacetylation degree were employed; ketoprofen, a non-steroidal anti- inflammatory drug, was chosen as the hydrophobic model drug. The multiple emulsion method produced well-formed microspheres with good yields. Acetic acid concentration in the polymeric solutions influenced particle size and drug content of the microspheres. The highest drug encapsulation efficiencies were obtained for the lowest theoretical drug/chitosan ratio.

Anti-Inflammatory Agents, Non-Steroidal↗

PubMedDate not supplied

Hyaluronidase-injectable microparticles intended for the treatment of extravasation.

Hyaluronidase is a protein whose enzymatic activity is successfully employed in extravasation therapy. Taking into account that several proteins (e.g. gelatin and albumin) have been employed as natural polymers for the preparation of microspheres, this work approaches a comprehensive investigation on hyaluronidase injectable microparticles. The goals are either to obtain a sustained release preparation of hyaluronidase or to use the enzyme as drug carrier. Microspheres have been prepared using a water-in-oil emulsification technique, and they have been crosslinked either by thermal or chemical means. Results show that hyaluronidase microspheres with good morphological characteristics can be obtained by this preparation method. Manufacturing variables influence the enzymatic activity of the microspheres, which can be highly preserved under mild experimental conditions. Moreover, the suitability of this enzyme as a microparticulate drug carrier has been shown by the successful encapsulation of hydrocortisone sodium succinate.

Animals↗