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.