2-Amino-4,6,7,8-tetrahydrothiopyrano[3,2-b]pyran-3-carbonitrile 5,5-dioxide VP-4535 as an antimicrobial agent selective toward methicillin‐resistant Staphylococcus aureus

The antibacterial activity of 2-amino-4,6,7,8-tetrahydrothiopyrano[3,2-b]pyran-3-carbonitrile 5,5-dioxide toward five key ESKAPE pathogenic bacteria, methicillin‐resistant Staphylococcus aureus (ATCC 43300), Escherichia coli (ATCC 25922), Klebsiella pneumonia (ATCC 700603), Acinetobacter baumannii (ATCC 19606), and Pseudomonas aeruginosa (ATCC 27853) was evaluated. The antifungal activity was studied­ towards pathogenic fungal strains Candida albicans (ATCC 90028) and Cryptococcus neoformans var. Grubii (ATCC 208821). Compound VP-4535 bearing 5-methylindolin-2-one motif possessed the highest antibacterial activity and excellent selectivity toward methicillin‐resistant Staphylococcus aureus but was inactive against non-resistant Staphylococcus aureus strain. The compound in therapeutic concentration was safe to human red blood cells, human lymphocytes, HaCaT, Balb/c 3T3 and HEK-293 cells

Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents

Development of a new effective drugs with low side effects and definite chemical characteristics needs indentification of bioactive scaffolds for further structural optimization. New synthesized derivatives of 4-hetaryl-5-amino-1-aryl-1H-1,2,3-triazoles and 3H-[1,2,3]triazolo[4,5-b]pyridines were tested for anticancer activity using 60 human tumor cell lines within 9 cancer types. The selective influence of (5-amino-1H-1,2,3-triazol-4-yl)quinazolin-4(3H)-ones: 2-(5-amino-1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)quinazolin-4(3H)-one and 2-(5-amino-1-phenyl-1H-1,2,3-triazol-4-yl)-6-bromoquinazolin-4(3H)-one on ovarian cancer OVCAR-4 cells with growth percentage (GP) = -4.08 and 6.63%, respectively, was found. The derivative 5,7-diamino-3-(3-(trifluoromethyl)phenyl)-3H-[1,2,3]triazolo[4,5-b]pyridine-6-carbonitrile possessed high activity towards lung cancer EKVX cells (GP = 29.14%). The compounds were shown to be less toxic than doxorubicin towards non-tumor human embryonic kidney cells of HEK293 line. Thus, the results of our study confirm the anticancer potential of compounds based on 5-amino-1-aryl-1H-1,2,3-triazoles scaffolds and their fused polycyclic derivatives

Diagnostyka silników elektrycznych na podstawie wyników pomiarów impedancji

There is proposed to estimate the engine state after it's impedance parameter measuring results obtaining. The vague pole engine replacement scheme and the measuring procedure are analyzed. The measuring parameters deviations from the corresponding parameters of the basic engine-models contain the information about the engine characteristics behavior. It makes possible to forecast the intensive working in harmony on-the-fly.W artykule omówiono ocenę stanu silnika na podstawie wyników pomiaru impedancji. Przeanalizowano schemat zastępczy niejawnobiegunowego silnika oraz metody pomiarowe. Odchylenia zmierzonych parametrów od odpowiadających im parametrów podstawowych modeli silnika zawierają informację o przebiegach charakterystyk silnika. W oparciu o omawianą metodę możliwe jest możliwe prognozowanie obciążeń silników