Synthesis of imidazoline and imidazo[2,1-c][1,2,4]triazole aryl derivatives containing the methylthio group as possible antibacterial agents.

1-Arylimidazolidine-2-thiones (1a-g) were synthesized by the condensation reaction of N-arylethylenediamines with carbon disulfide in xylene medium. Their further alkylation with methyl iodide led to the formation of some biologically active 1-aryl-2-methylthio-imidazolines (2a-g). The 7-(4-methylphenyl)-3-methylthio-5H-6,7-dihydroimidazo[2,1-c][1,2,4]triazole (4b) was obtained by the alkylation of the respective 7-(4-methylphenyl)-2,5,6,7-tetrahydroimidazo[2,1-c][1,2,4]triazol-3(H)-thione (3b) with methyl iodide.

Exclusion of antimicrobial activity of some analgesic active imidazo[2,1-c][1,2,4]triazines.

The purpose of this study was to exclude the potential antimicrobial activity of certain analgesic active imidazo[2,1-c][1,2,4]triazines. These compounds contain in their chemical structure potential pharmacophore formations and features similar to those present in morphine-like analgesics and opioid receptor agonists containing no basic nitrogen atom. These compounds showed significant antinociceptive activity on central nervous system of tested animals, correlated with relatively low acute toxicity values (LD50 in range from 1100 to above 2000 mg kg(-1) b.

Antimicrobial screening of certain fused 1,2,4-triazine derivatives.

The synthesized fused 1,2,4-triazines were tested for their potential antimicrobial activity resulting from the literature data. Microbiological screening tests conducted in relation to 54 strains of Gram-positive and 52 strains of Gram-negative bacteria, 6 strains of yeast-like fungi and 3 strains of moulds showed that these compounds in examined concentrations 100 mg ml(-1) and 200 mg ml(-1) had no influence on the growth of microorganisms tested. The microbiological screening tests afforded to limit the possible biological spectrum of activity of tested compounds.

The susceptibility of certain microbial strains to fused 1,2,4-triazole derivatives.

1,2,4-Triazole is the structural element of many drugs that have different pharmacological spectrum of activity. Besides, from the literature data it follows that 1,2,4-triazoles and its fused systems show antibacterial, antifungal and anti-inflammatory activities. The obtained compounds were tested for their potential antimicrobial activity.

The susceptibility of certain bacterial strains to imidazotriazine derivatives.

The synthesized imidazo[2,1-c]triazines were tested for their antimicrobial activity. Microbiological screening tests conducted in relation to 54 strains of Gram-positive and 52 strains of Gram-negative bacteria, 6 strains of yeast-like fungi and 3 strains of moulds showed significant activity of compound 19 against 52 Gram-negative bacterial strains. This compound was active against 16 strains of Escherichia coli, 12 strains of Pseudomonas, 10 strains of Proteus spp.