3H-[1,2]Dithiolo[3,4-b]pyridine-3-thione and its derivatives synthesis and antimicrobial activity.

A series of 2-substituted isothiazolo[5,4-b]pyridine-3(2H)-thiones, isothiazolo[5,4-b]pyridin-3(2H)-ones, N-substituted 2-sulfanylnicotinamides and the corresponding carbothioamide derivatives were synthesized and evaluated for their antimicrobial activity against several strains of Gram+ and Gram- bacteria and fungi. Chemical syntheses were resumed into a comprehensive cyclic route that enables the reversible conversion for each derivative of the series considered. Among the tested compounds the N-(aralkyl)-2-sulfanylnicotinamides show the highest fungitoxicity (MIC = 1.

Antimicrobial and genotoxic activities of N-hydroxyalkyl-1, 2-benzisothiazol-3(2H)-one carbamic esters.

N-Hydroxyethyl- and N-hydroxypropyl-1,2-benzisothiazol-3(2H)-one carbamic esters were prepared in order to test their activity against representative bacterial and fungal strains. The obtained results were compared with those reported for parent alcohols and some interesting considerations were drawn. None of the studied derivatives possess genotoxic activity in the Bacillus subtilis rec-assay and Salmonella-microsome test.

In vitro anti-Mycobacterium avium activity of N-(2-hydroxyethyl)-1,2-benzisothiazol-3(2H)-one and -thione carbamic esters.

A series of N-(2-hydroxyethyl)-1,2-benzisothiazol-3(2H)-one and -thione carbamic esters have been synthesised and tested against Mycobacterium avium strains. The MIC values determined by the radiometric broth dilution method were between 2 and 8 micrograms/mliters for the benzisothiazolthione derivatives and between 16 and 32 micrograms/mliters or higher for the corresponding benzisothiazolone derivatives.

[Phytotoxic activity of N,N-di-sec-butylbenzamides with alkyl substituents on the aromatic nucleus].

A new series of N,N-di,sec.butylalkylbenzamides was studied and it was found that some compounds showed particularly interesting selective phytotoxicity comparable with that shown by analogous halogen derivatives.

[Phytotoxic activity of asymmetric N,N-dialkylamides of trisubstituted benzoic acids].

Asimmetric N,N-dialkylamides of benzoic acids variously trisubstituted on the nucleus were prepared and tested for phytotoxicity in pre- and post-emergence experiments. These amides are characterized by the presence on the amidic N of a sec.butyl or a 1-methylbutyl or a 1-ethylpropyl group and a second alkyl group of varying weight and nature.

[Preparation and study of the phytotoxic activity of arylalkylamides. II. N-Phenethylamides].

A series of N-phenetylamides was prepared and tested for phytotoxic activity. Comparison with N-benzylamides showed that lengthening the alkyl chain in the aralkylamide residue reduces phytotoxicity and that, also in the case of phenetylamides, phytotoxic activity is not due to inhibition of the Hill reaction.

[2-amino-3,5-dichloro-benzoic acid and 3-amino-2,5-dichloro-benzoic acid derivatives with phytotoxic action].

Derivatives of 2-amino-3,5-dichloro- and 3-amino-2,5-dichlorobenzoic acids have been prepared in order to extend previous research regarding the phytotoxicity of these two acids and of the corresponding N,N-di,sec.butylamides. The methyl esters of the two acids, the corresponding acids acetylated on the amino group and their respective methyl esters, and the N,N-di,sec.

[Preparation and study of phytotoxicity of N-arylalkyl substituted amides. I. Benzylamides].

A series of N-benzyl substituted amides (substances I-CV) have been prepared and tested for phytotoxicity. Preliminary tests were carried out on various common plants using both pre- and post-emergence tests at doses of 6 kg/ha. Further tests using doses of 4 and 2 kg/ha were carried out on the most interesting compounds.

[Preparation and study of phytotoxic activity of anilides of the (+/-) hydratropic acid].

A series of ((+/-)-hydratropanilides variously substituted in the aniline nucleus (substances I leads to XXXIX) were prepared. The substances were studied for inhibition of the Hill reaction and for phytotoxicity. Comparison of the results of in vitro and in vivo tests did not often show strict correlation of data: in particular it seems probable that in the hydratropanilide series substances active on the isolated chloroplast are hindered in vivo in the absorption and transport phases and thus cannot reach the receptor sites.

[Alkylthiophenylureas with phytotoxic activity].

A series of 1-(p.alkylthio)phenylureas variously substituted on the N atom in position 3 (substances I leads to XXXVII) has been prepared and studied for pre- and post-emergence phytotoxicity. Some compounds were found to have high activity; in particular some 1-(p.