21719-55-1Relevant academic research and scientific papers
Synthesis of 1,6-hexanediyl-bis(semicarbazides) and 1,6-hexanediyl-bis(1,2, 4-triazol-5-ones) and their antiproliferative and antimicrobial activity
Pitucha, Monika,Rzymowska, Jolanta,Olender, Alina,Grzybowska-Szatkowska, Ludmia
, p. 1 - 8 (2012)
A series of 1,6-bis(3-substituted 1,5-dihydro-5-oxo-4H-1,2,4-triazol- -4-yl)hexanes 3a-g were synthesized by the cyclization reaction of 1,6-bis{[(2- -substituted hydrazinyl)carbonyl]amino}hexanes 2a-g in alkaline medium. The new derivatives 3a-c were screened in vitro for their antiproliferative and anticancer activity in human tumor cell lines derived from breast and lung carcinoma cells. Compounds 3a (at a concentration of 0.18 mM), 3b (at concentrations of 0.12 and 0.02 mM) and 3c (at concentrations of 0.23 and 0.11 mM) were found to be the most effective against the lung cell line. Compound 3a had the greatest antiproliferative effect on the breast carcinoma cell line. Representative compounds were established and evaluated as antimicrobial agents. All the tested derivatives showed minimum inhibitory concentrations (MIC) in the range 1.87-7.5 μg mL-1. Compound 3b was the most effective against Candida albicans (MIC 1.87 μg mL-1). Copyright 2012 (CC) SCS.
Antioxidant evaluation of some semicarbazide, 1,2,4-triazolone and pyrazolone derivatives
Pitucha, Monika,Nowak, Renata
experimental part, p. 1004 - 1008 (2012/07/03)
1,2,4-Triazoles, pyrazoles and semicarbazides possessing heterocyclic ring 1-14 were synthesized as compounds with interesting pharmacological profiles. All were investigated in vitro for their antioxidant activity. Some compounds showed significant effect in the above assay. The most promising was a group of pyrazolone. The effect was dependent mainly on the substituent on the amide group. It was found that compounds 8 and 10 showed the highest antioxidant capacity comparable with the widely used reference, antioxidant 6-hydroxy-2,5,7,8- tetramethylchroman-2-carboxylic acid (Trolox).
