Gustavo Luiz Paraginski

In vitro evaluation of triazenes: DNA cleavage, antibacterial activity and cytotoxicity against acute myeloid leukemia cells

). The observation of intermolecular hydrogen bonding in the solid state of compound 3, based on the structural analysis by X-ray crystallography, as well as the results of IR and UV-Vis spectroscopic analyses of compounds 1, 2 and 3 are discussed in the present work.

Triazenos e atividade antibacteriana

Fifteen triazenes compounds were studied concerning their antibacterial activity by broth microdilution method. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) was determined with E. coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Acinetobacter baumannii, Acinetobacter lwoffii, Ralstonia pickettii, Bordetella bronchiseptica, Micrococcus sp., Enterococcus sp., Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae, Bacillus cereus, Corynebacterium sp., Rhodococcus sp., Salmonella sp., Serratia marcescens, Morganella morganii, Enterobacter cloacae, Shigella flexneri, Shigella sonnei, Shigella sp., Klebsiella pneumoniae, ESBL Klebsiella oxytoca 14, ESBL Klebsiella pneumoniae 23, ESBL Klebsiella pneumoniae 24, ESBL Klebsiella pneumoniae 25, ESBL Escherichia coli 26, ESBL Klebsiella pneumoniae 27, ESBL Klebsiella pneumoniae 31, ESBL Escherichia coli 32, ESBL Klebsiella pneumoniae 37 e ESBL Escherichia coli 38. The highest effect was evidenced by the compound 1-methyl-3-(p-carboxyphenyl)triazene 1-oxide (2) against Streptococcus agalactiae (MIC = 16 µg/mL and MBC = 32 µg/mL). The compounds 1-phenyl-3-(4-nitrophenyl)triazene-1-oxide (9), 1-(4-nitrophenyl)-3-(4-carboxyphenyl)triazene (10) e 1-(4-acethyl amine phenyl)-3-(4-carboxyphenyl)triazene (11) presented MIC between 32 and 64 µg/mL against S. edipermidis, S. saprophyticus, Rhodococcus sp. and E. cloacae. The compounds 1-methyl-3-phenyltriazene-1-oxide (1) , bis-1,3-(4-acethyl oxime)triazene (3), bis-1,3 (4-acethyl phenyl)triazene (4), 1-(2-fluorophenyl)-3-(4-acethylphenyl)triazene (5), 1,3-(3-hydroxy-diphenyltriazenide)(piridil)(bis-oxo-vanadium) (12), 1-(3-nitrophenyl)-3-phenyltriazene (14), 1-(4-nitrophenyl)-3-benzyltriazene (15) presented MIC of the 128 µg/mL against S. aureus ATCC 25923, P. aeruginosa ATCC 27853, A. lwoffii, Micrococcus sp., S. epidermidis, S. saprophyticus, Corynebacterirum sp., E. cloacae, S. flenneri e S. sonnei. The compounds 1-phenyl-3-(4-acethylphenyl)triazene (6), 1,3-bis-(4-ethoxycarbonylphenyl) triazene (7), and 3-(4-carboxylatephenyl)-1-methyltriazene 1-oxide of potassium tetrahydrate (13) presented MICs equals or highest than 128 µg/mL. The results have demonstrated the potential biological activity of these compounds against Gram-positive and Gram-negative bacteria.

Atividade antibacteriana in vitro e toxicidade frente à Artemia salina Leach. de alguns compostos triazenos

Bacterial resistance to antibacterial agents is currently a major concern. We report the synthesis, in vitro antibacterial activity and toxicity toward Artemia salina of six diaryltriazene compounds bearing different substituent groups. Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) values against standard strains (ATCC) and clinical isolates (including ESBL, MBL and AmpC strains) were good to very good, in the range 8 to 128 mg mL-1. Results suggest that hydroxyl, 4-carboxyl and 4-phenyldiazenil groups attached to the diaryltriazenes provide enhanced activity. Toxicity results showed very low LC50 values for three compounds (10-fold lower than DTIC).

IN VITROANTIBACTERIAL ACTIVITY AND TOXICITY TOWARDArtemia salinaLeach. OF SOME TRIAZENE COMPOUNDS

Bacterial resistance to antibacterial agents is currently a major concern. We report the synthesis, in vitro antibacterial activity and toxicity toward Artemia salina of six diaryltriazene compounds bearing different substituent groups. Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) values against standard strains (ATCC) and clinical isolates (including ESBL, MBL and AmpC strains) were good to very good, in the range 8 to 128 mg mL-1. Results suggest that hydroxyl, 4-carboxyl and 4-phenyldiazenil groups attached to the diaryltriazenes provide enhanced activity. Toxicity results showed very low LC50 values for three compounds (10-fold lower than DTIC).