Synthesis and Biological Evaluation of New 3-Phenyl-1-[(4-arylpiperazin-1-yl)alkyl]-piperidine-2,6-diones

A set of 13 alkyl derivatives of 3-phenylpiperidine-2,6-dione were synthesized. Newly obtained compounds were investigated in vitro against HIV-1 and other selected viruses. The benzyl 3f and fluorophenyl 3g derivatives showed moderate protection against CVB-2 and the compound 3g also against HSV-1. Derivatives were tested also for their antibacterial and antifungal activity. The molecular structures of 3a and 3d were determined by an X-ray analysis

The cytotoxic effect of copper (II) complexes with halogenated 1,3-disubstituted arylthioureas on cancer and bacterial cells

A series of eight copper (II) complexes with 3-(4-chloro-3-nitrophenyl)thiourea were designed and synthesized. The cytotoxic activity of all compounds was assessed in three human cancer cell lines (SW480, SW620, PC3) and human normal keratinocytes (HaCaT). The complexes 1, 3, 5, 7 and 8 were cytotoxic to the studied tumor cells in the low micromolar range, without affecting the normal cells. The complexes 1, 3, 7 and 8 induced lactate dehydrogenase (LDH) release in all cancer cell lines, but not in the HaCaT cells. They provoked early apoptosis in pathological cells, especially in SW480 and PC3 cells. The ability of compounds 1, 3, 7 and 8 to diminish interleukin-6 (IL-6) concentration in a cell was established. For the first time, the influence of the most promising Cu (II) complexes on intensities of detoxifying and reactive oxygen species (ROS) scavenging the enzymes of tumor cells was studied. The cytotoxic effect of all copper (II) conjugates against standard and hospital bacterial strains was also proved

Antistaphylococcal Activity of Selected Thiourea Derivatives

Five of thiourea derivatives were prepared using as a starting compound 3-(trifluoromethyl)aniline, 4-chloro-3-nitroaniline, 1,3-thiazol-2-amine, 2H-1,2,3-triazol-4-amine and commercial isothiocyanates. All compounds were evaluated in vitro for antimicrobial activity. Derivatives 2 and 3 showed the highest inhibition against Gram-positive cocci (standard and hospital strains). The observed MIC values were in the range of 0.5–8 μg/ml. The products effectively inhibited the formation of biofilms of methicillin-resistant and standard strains of Staphylococcus epidermidis. Inhibitory activity of thioureas 2 and 3 against Staphylococcus aureus topoisomerase IV was studied. The examined compounds were nongenotoxic

Biological evaluation of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives

AbstractAntibacterial and antifungal activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives were examined by the disc-diffusion method (growth inhibition zone diameter in agar medium). The MIC's for the most active agents were determined. Title compounds were also evaluated in vitro against representatives of different virus classes. Most of the tested compounds exhibit activity against CVB-2 virus

9-Methyl-3,5-dioxo-4-azatricyclo[5.2.2.02,6]undec-8-ene-1,8-diyl Diacetate

9-Methyl-3,5-dioxo-4-azatricyclo[5.2.2.02,6]undec-8-ene-1,8-diyl diacetatewas synthesized from 2-methylcyclohexane-1,3-dione and 1H-pyrrole-2,5-dione. The title compound was characterized by 1H NMR, 13C NMR, elemental analysis and MS

Decentralized fault location, isolation and self restoration (FLISR) logic implementation using IEC 61850 GOOSE signals

Fault location, isolation and self-restoration (FLISR) automation is an essential component of smart grids concept. It consists of a high level of comprehensive automation and monitoring of the distribution grid improving the quality of energy supplied to customers. This paper presents an algorithm for decentralized FLISR architecture with peer-to-peer communication using IEC 61860 GOOSE messages. An analysis of short circuit detection was presented due to the method of the grid earthing system. The proposed automation model was built based on communication logic between configured intelligent electronic devices (IED) from ABB and Siemens. The laboratory tests were conducted in a half-loop grid model with a bilateral power supply (typical urban grid). The laboratory research concerned three locations of short circuits: between substation and section point, between two section points and between section point and normally open point (NOP). The logic implementation was developed using State Sequencer software offered by Test Universe