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Biomedical subjects

M Mazza

Publications and source records attributed to M Mazza.

At least 73 records · Page 4Linked 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 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↗
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↗
PubMed1978

[Phytotoxicity of di,sec.butylamides of halogenoalkoxybenzoic acids].

N,N-di,sec.butylamides of halogenated alkoxybenzoic acids were prepared and tested for phytotoxic activity. The corresponding acids and a series of N-alkyl- and N,N-dialkylamides of 2-methoxy-3,5-dichlorobenzoic acid were studied in parallel. The phytotoxicity of these substances was tested against seven representative weeds and some crop plants using both pre- and post-emergence test at doses of 6 kg/ha or lower. The amides studied proved more strongly phytotoxic on absorption through the root than through the foliage. Furthermore selective phytotoxic activity against two important infesting graminacae, Echinochloa crus-galli R.S. and Setaria glauca L. was observed. Some of these compounds showed low toxicity or were tolerated by crop plants. The results obtained with this series of amides of 2-methoxy-3,5-dichlorobenzoic acid confirm the importance of the sec.butyl group on N for the appearance of selective phytotoxicity.

Benzoates↗
PubMed1978

[Selective phytotoxic activity of N,N-di,sec.butylamides of aminobenzoic acids mono-, di- and tri-substituted on the nucleus].

N,N-di,sec.butylaminobenzamides, mono-, di- or trisubstituted on the nucleus with methyl and/or halogen groups were prepared and tested for phytotoxicity. The corresponding benzoic acids and series of N-alkyl- and N,N-dialkylamides of 2-amino-3-bromo-5-methyl-, 2-amino-3,5-dibromo, 2-amino-3,5-dichloro- and 3-amino-2,5-dichlorobenzoic acids were studied in parallel. Both pre- and post-emergence phytotoxicity tests were carried out with doses of 6 kg/ha or less on seven representative weeds and some plants of agricultural interest. The series of N,N-di,sec.butylamides studied proved to be effectively phytotoxic on absorption through either the roots or the foliage. As regards the effect of substitution in the nucleus on the phytotoxicity of these amides, 3,5-dihalogenation proved important. The results also showed: 1) the importance of two sec.butyl groups on the amide nitrogen for the appearance of selective phytotoxicity against two grass weeds; 2) the different behaviour of the two acids (XXIa) and (XXIIa) in comparison with the corresponding di,sec.butylamides (XXI) and (XXII); 3) the importance of derivative (IL) which was highly active against graminaceous weeds but showed low phytotoxicity against crop plants, graminaceous ones included.

Aminobenzoates↗
PubMed1977

Primary amides of bis-(2-carboxyphenyl)-disulfides with antimycotic activity.

A series of bis-amides of 2,2'-dicarboxydiphenyldisulfides with monosubstituted N-alkyl groups (substances I leads to XXVI) or N-aralkyl groups (substances XXVI leads to XLII) was prepared and examined for in vitro antifungal activity. The substances were obtained by condensing the chloride of 2,2'-dicarboxydiphenyldisulfide with suitable amines. The fungistatic activity of the products was tested in vitro against the following four strains: Candida albicans, Candida tropicalis, Saccharomyces cerevisiae, Trichophyton mentagrophytes. The results obtained summarised in Tables I and II amplify the structure-antifungal activity relationships of this class of compound. The most active compounds proved to be bis-(N-n.heptyl-2-carboxami-dophenyl)disulfide (XX) and bis-(N-beta-4Cl-phenylethyl-2-carboxamidophenyl)disulfide (XXXV).

Antifungal Agents↗
PubMed1977

[N-acylindoline with phytotoxic activity. II].

A series of N-acyl derivatives of indoline (A) was prepared and studied for phytotoxic activity. The substances studied (Tables I and II, substanes I leads to XXXVIII) were mostly new compounds and were prepared from the appropriate indoline by condensation with acid chlorides and isocyanates. The biological tests consisted in pre- and post-emergence treatment in doses of 6 kg/ha or less of six common weeds and for two substances (XVIII, XIX) of other species of agricultural importance (Table III). The results show that N-methylcarbamoyl and N-dimethylcarbamoylindolines in which the indoline nucleus bears a halogen or alkyl substituent are highly active on absorption via the roots of foliage and have a wide spectrum of action. The compounds showing the highest phytotoxic activity in both pre- and post-emergence tests were 5Cl-N-(methylcarbamoyl)indoline (XVIII), 5Cl-N-(dimethylcarbamoyl)indoline (XIX) and 2CH3-N-(methylcarbamoyl) indoline (XXXIII).

Chemical Phenomena↗
PubMed1977

[On the phytotoxicity of some N 1-phenyl-N 1- alkylureas].

A series of N1-phenyl-N1-alkylureas (E) and a series of N-carbamoyl derivatives of tetrahydroquinoline (D) were prepared and studied for phytotoxicity. The substances studied (Tables I, II, substances i leads to xxvii) were mostly new compounds and were prepared from suitable secondary amines by condensation with alkylating agents. Biological tests involved pre- and post-emergence treatment of five common weeds with doses of 6 kg/ha and lower doses (Tables i, ii). The tetrahydroquinoline derivatives (I leads to VII) proved inactive except for the N-dimethylcarbamoyl derivative (III) which on foliar absorption showed selective phytotoxicity against Vicia sativa L. Most of the members of the N1-phenyl-N1-alkylurea class (VIII leads to XXVII) did not have wide spectrum phytotoxicity. Some compounds have however interesting specificity of action against Vicia sativa L.

Alkylation↗
PubMed1976

[Phytotoxicity of hydrazones of aromatic aldehydes].

A series of hydrazones of aromatic aldehydes (B) was prepared and tested for phytotoxicity. These compounds are bioisosters of 1-aryltriazenes (A) which were found to possess interesting phytotoxic properties in a previous research. The substances studied (Tables I leads to III: compounds(I leads to CLXXX)) some of which were previously unrecorded, were prepared by the usual procedures from the required aldehyde and hydrazine derivative. The phytotoxicity of all the compounds was studied using seven representative species in both pre- and post-emergence tests at a dose of 6 kg/ha. It was found that this class of compounds shows phytotoxicity by absorption through the foliage with specificity for Amaranthus retroflexus L. The only exceptions are compounds where the aryl residue is 2,6-dichlorophenyl; these compounds show wide spectrum of phytotoxicity by absorption through the leaves.

Aldehydes↗
PubMed1976

[N-acylindoline with phytotoxic activity. I].

A series of N-acyl derivatives of indoline (A) was prepared and tested for phytotoxic activity. The substances studied (Tables I leads to III, substances I leads to XXVIII) were prepared by reaction of indoline with suitable acylating agents and were mainly new compounds. The biological tests consisted in pre- and post-emergence treatment in doses of 6 kg/ha or lower doses on five common weeds; one substance (XXV) was tested also on other species of economic importance (Table III). The results show that of the three classes studied the N-carbamoyl- and N-thiocarbamoyl derivatives of indoline have wide spectrum phytotoxic activity especialy on absorption via the foliage. The highest phytotoxic activity in both pre- and post-emergence tests was shown by N-(methylcarbamoyl)indoline (XIII) and N-(dimethylcarbamoyl(indoline (XXIII).

Acylation↗
PubMed1976

[Phytotoxic activity of triazene derivatives. VI. 1-aryl-3-arylalkyl-3-alkyltriazene derivatives].

A series of of 1-aryl-3-arylalkyl-3-alkyltriazenes (B) was prepared and studied for phytotoxic activity. The previously unknown substances [Table I: substances (I leads to XVI)] were prepared by condensation of the appropriate diazonium salt with the required secondary amine in an alkaline medium and were tested against five representative plant species in both pre- and post-emergence tests at a dose of 6 kg/ha. All the substances studied were inactive in pre-emergence tests. However most of the compounds showed phytotoxic activity by absorption through the foliage. This activity was not very pronounced and always lower than triazene analogs previously studied (type A compounds) which have no aralkyl residue on nitrogen 3.

Herbicides↗