Wyniki wyszukiwania - Biblioteka Nauki

1

Synthesis and pharmacological evaluation of some novel thiourea derivatives incorporating 3-(trifluoromethyl)phenyl moiety

100%

Kedzierska E. , Fidecka S. , Bielenica A. , Struga M.

Acta Neurobiologiae Experimentalis

|

2014

|

tom 74

|

nr 3

EN

Despite the great progress in the treatment of pain, depression, anxiety, and other central nervous system (CNS) disorders, the used drugs do not fulfil all expectations. And there is still a need to search for new, more effective therapies as well as need to know the mechanisms of action of existing drugs. The tested compounds are a group of thiourea derivatives with expected potential central activity in the CNS. Numerous thiourea-derived compounds are selective ligands for 5-HT2 receptors family (Forbes et al. 1995) and also exhibit a broad spectrum of biological activities as analgesic, antidepressant, anticonvulsant, antiviral, anti-HIV, antibacterial, and HDL-elevating properties (Struga et al. 2007, Wardakhan et al. 2008, Karakus et al. 2009). Modification of the chemical structure makes it possible to obtain new compounds with pharmacological activity, higher selectivity and fewer adverse effects. Compounds were studied in behavioral tests used to predict a potential influence on the CNS in mice (after their ip or sc administration). The results of the pharmacological studies showed that new compounds exerted substantial impact on the CNS in mice. The most important seems to be their influence on the transmission of serotonin (activity in the head-twitch test, changes in body temperature) as well as antinociceptive effects. These compounds caused no coordination disorders, and do not affect locomotor activity, but slightly decreased the hyperactivity caused by administration of amphetamine. Obtained results indicate the possibility of the involvement of serotonin in the action of the majority of the compounds.

2

Biological evaluation of quaternary bis ammonium salt and cetylpyridinum bromide against S. epidermidis biofilm

88%

Stefanska J. , Pietruczuk-Padzik A. , Struga M. , Borkowski M. , Tyski S.

Polish Journal of Microbiology

|

2013

|

tom 62

|

nr 4

EN

Quaternary ammonium compounds are broad-spectrum bacteriocides widely used as antiseptics, disinfection and preservation agents. The aim of this study was to examine the activity of two quaternary ammonium salts, cetylpyridinum bromide and a newly synthesized quaternary bis ammonium salt, against S. epidermidis biofilm. The average values of killing efficiency for cetylpyridinum bromide ranged from 26.6% to 64.1% for all tested concentrations (0.125 to 8.0 μg×mL⁻¹) and for quaternary bis ammonium salt the percentage of killing efficiency ranged from 59.7% to 88.4% for tested concentrations (from 2.0 to 128.0 μg×mL⁻¹). Both tested compounds significantly affect staphylococcal biofilms, but any of used concentrations caused a total eradication of bacterial biofilm.

3

Antistaphylococcal activity of selected thiourea derivatives

88%

Stefanska J. , Stepien K. , Bielenica A. , Wrzosek M. , Struga M.

Polish Journal of Microbiology

|

2016

|

tom 65

|

nr 4

EN

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.

4

Antimicrobial activity of 2,4-dihydro-[1,2,4]triazol-3-one derivatives

88%

Stefanska J. , Struga M. , Tyski S. , Kossakowski J. , Dobosz M.

Polish Journal of Microbiology

|

2008

|

tom 57

|

nr 2

EN

Antibacterial and antifungal activity of 2,4-dihydro-[1,2,4]triazol-3-one 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. Of all the tested compounds, aminomethy1 derivatives of 2,4-dihydro-[1,2,4]triazol-3-one exhibit activity against the majority of microorganisms studied.