The present study is focused on the synthesis and investigation of the physicochemical and biological properties of silver nanoparticles stabilized with a series of cationic gemini surfactants having a polymethylene spacer of variable length. UV-VIS spectroscopy, dynamic light scattering, scanning electron microscopy and zeta potential measurements were applied to provide physicochemical characterization of the silver nanoparticles. The mean size values of the nanoparticles were found to be in the 50 to 115 nm range. From the nanoparticle size distributions and scanning electron microscopy images it results that a population of small nanoparticles with the size of several nanometers was confirmed if the nanoparticles were stabilized with gemini molecules with either a short methylene spacer (two or four -CH₂- groups) or a long spacer (12 -CH₂- groups). The average zeta potential value for silver nanoparticles stabilized with gemini molecules is roughly independent of gemini surfactant spacer length and is approx. +58 mV. An interaction model between silver nanoparticles and gemini molecules which reflects the gained experimental data, is suggested. Microbicidal activity determinations revealed that the silver nanoparticles stabilized with gemini surfactants are more efficient against Gram-negative bacteria and yeasts, which has a direct relation to the interaction mechanism of nanoparticles with the bacterial cell membrane and its structural composition.

• Klíčová slova
• gemini surfactant, microbicidal activity, nanoparticle stability, silver nanoparticle, surfactant spacer,
• MeSH
• antiinfekční látky farmakologie   MeSH
• gramnegativní bakterie účinky léků   MeSH
• houby účinky léků   MeSH
• kovové nanočástice chemie   MeSH
• micely MeSH
• povrchově aktivní látky chemie   MeSH
• stříbro chemie   MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antiinfekční látky MeSH
• micely MeSH
• povrchově aktivní látky MeSH
• stříbro MeSH

The aim of this study was to test efficacy of a newly developed foam disinfectant Hvĕzda S.C.H. using the standard procedures. The agent was initially intended for use as a detoxicant for the needs of the Army, Integrated Rescue System and Fire and Rescue Service of the Czech Republic and its active ingredient is hydrogen peroxide. Microbicidal efficacy of the agent was tested under the conditions required by the standards for the evaluation of bactericidal, fungicidal, sporicidal, mycobactericidal and virucidal activity of chemical disinfectants and antiseptics in health care settings, food, industrial, domestic and institutional areas and veterinary care facilities. In all of the efficacy tests used, the foam disinfectant Hvĕzda S.C.H. reduced density of test microorganisms under the prescribed conditions by at least eight orders of magnitude, even for much shorter exposure times (1, 5, 10 minutes) than usually prescribed by the standards. In conclusion, the foam disinfectant Hvĕzda S.C.H. easily met the requirements for the bactericidal, fungicidal, sporicidal, mycobactericidal and virucidal activity, with a reserve of several orders of magnitude, under the conditions prescribed by the standards for health care, community and veterinary settings.

• MeSH
• dezinficiencia farmakologie   MeSH
• mikrobiální testy citlivosti * MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• dezinficiencia MeSH

3-[4-(Substituted)phenyl-/4-(diphenylmethyl)phenylpiperazin-1-yl]-2-hydroxypropyl-1-[(substituted)phenyl]carbamates and their salts with hydrochloric acid were synthesized, characterized, and tested in vitro against Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 as reference and quality control strains, against three methicillin-resistant isolates of S. aureus, and three isolates of vancomycin-resistant E. faecalis. All the compounds were evaluated against Mycobacterium tuberculosis H37Ra/ATCC 25177, M. kansasii DSM 44162, and M. smegmatis ATCC 700084. All of the tested compounds demonstrated very good activity against all the tested strains/isolates comparable with or better than that of clinically used drugs (ampicillin, ciprofloxacin, vancomycin, isoniazid). 1-[{(3-Trifluoromethyl)phenyl}carbamoyloxy-2-hydroxypropyl]-4-(3,4-dichlorophenyl)piperazin-1-ium chloride demonstrated the highest potency against all the tested strains/isolates (MICs ranged from 3.78 to 30.2 µM), and 1-[{(3-trifluoromethyl)phenyl}carbamoyloxy-2-hydroxypropyl]-4-(diphenylmethyl)piperazin-1-ium chloride was the most effective against all the screened mycobacterial strains (MICs ranged from 3.64 to 14.5 µM). All the investigated derivatives had strong antibiofilm activity against S. aureus ATCC 29123 and a synergistic or additive effect with gentamicin against isolates of E. faecalis with both intrinsic and acquired resistance to gentamicin. The screening of the cytotoxicity of the compounds was performed using human monocytic leukemia THP-1 cells. The IC50 values of the most effective compounds ranged from ca. 2.8 to 7.3 µM; thus, it can be stated that the antimicrobial effect is closely connected with their cytotoxicity. These observations disqualify these compounds from further development as antimicrobial agents, but they can be considered potential multi-target drugs with a preferred anticancer effect with good water solubility and additional anti-infectious activity.

• Klíčová slova
• Antibacterial, Antibiofilm activity, Antimycobacterial, Antiproliferative effect, Carbamate, Piperazine, Synergy,
• MeSH
• antiinfekční látky farmakologie   terapeutické užití   MeSH
• karbamáty farmakologie   terapeutické užití   MeSH
• lidé MeSH
• piperaziny farmakologie   terapeutické užití   MeSH
• vztahy mezi strukturou a aktivitou MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• antiinfekční látky MeSH
• karbamáty MeSH
• piperaziny MeSH

A set of 4-benzylsulfanyl derivatives of pyridine-2-carbonitriles and pyridine-2-carbothioamides, previously tested for their antimycobacterial activity, were analysed by quantitative structure-activity relationship (QSAR) techniques, using some physicochemical and quantum-chemical parameters. The resulting QSAR revealed that the activity increases with electron withdrawing substituents in the benzyl moiety of studied compounds. HOMO orbitals can play an important role in the description of the mechanism of interactions at the molecular level. Additionally, the results of multiple linear regression indicate the differences between Mycobacterium tuberculosis and M. avium. The hydrophobicity of studied compounds is important for activity against M. avium.

• MeSH
• antiinfekční látky farmakologie   MeSH
• kvantitativní vztahy mezi strukturou a aktivitou * MeSH
• molekulární modely MeSH
• pyridiny farmakologie   MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• antiinfekční látky MeSH
• pyridiny MeSH

Twenty-four 2-(4-oxo-2-thioxothiazolidin-3-yl)acetic acid (rhodanine-3-acetic acid)-based amides, esters and 5-arylalkylidene derivatives were synthesized, characterized and evaluated as potential antimicrobial agents against a panel of bacteria, mycobacteria and fungi. All of the derivatives were active against mycobacteria. N-(4-Chlorophenyl)-2-[5-(2-hydroxybenzylidene)-4-oxo-2-thioxothiazolidin-3-yl]acetamide demonstrated the highest activity against Mycobacterium tuberculosis with minimum inhibitory concentrations (MIC) of 8-16μM. Non-tuberculous mycobacteria were the most susceptible to 2-[5-(2-hydroxybenzylidene)-4-oxo-2-thioxothiazolidin-3-yl]acetic acids (MIC values ⩾32μM). The highest antibacterial activity against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus exhibited 4-(trifluoromethyl)phenyl 2-(4-oxo-2-thioxothiazolidin-3-yl)acetate (MIC⩾15.62μM). Several structure-activity relationships were identified. The activity against Gram-negative and fungal pathogens was marginal.

• Klíčová slova
• 2-(4-Oxo-2-thioxothiazolidin-3-yl)acetic acid, Amides, Antibacterial activity, Antifungal activity, Antimycobacterial activity, Condensation, Esters, In vitro activity, Rhodanine,
• MeSH
• antiinfekční látky farmakologie   MeSH
• Candida účinky léků   MeSH
• grampozitivní bakterie účinky léků   MeSH
• kyselina octová chemie   MeSH
• magnetická rezonanční spektroskopie s uhlíkem 13C MeSH
• methicilin rezistentní Staphylococcus aureus účinky léků   MeSH
• mikrobiální testy citlivosti MeSH
• protonová magnetická rezonanční spektroskopie MeSH
• rhodanin chemie   farmakologie   MeSH
• spektrofotometrie infračervená MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antiinfekční látky MeSH
• kyselina octová MeSH
• rhodanin MeSH

New quaternary ammonium salt-type compounds with lipophilic cholesterol and terpene moieties were synthesized. The compounds showed promising antibacterial and antimycobacterial activities. Those compounds containing the cholesterol moiety showed significant activity against Staphylococcus aureus, Staphylococcus epidermidis, and Enterococcus faecium. On the contrary, the antimycobacterial activity increased with the presence of the terpene unit in the molecule.

• Klíčová slova
• Antibacterial activity, Antifungal activity, Cholesterol, Terpenes, Tuberculostatics,
• MeSH
• antiinfekční látky chemická syntéza   farmakologie   MeSH
• cholesterol analogy a deriváty   chemická syntéza   farmakologie   MeSH
• Enterococcus faecium účinky léků   růst a vývoj   MeSH
• houby účinky léků   růst a vývoj   MeSH
• kvartérní amoniové sloučeniny chemická syntéza   farmakologie   MeSH
• mikrobiální testy citlivosti MeSH
• molekulární struktura MeSH
• Mycobacterium účinky léků   růst a vývoj   MeSH
• racionální návrh léčiv MeSH
• Staphylococcus aureus účinky léků   růst a vývoj   MeSH
• Staphylococcus epidermidis účinky léků   růst a vývoj   MeSH
• terpeny farmakologie   MeSH
• vztahy mezi strukturou a aktivitou MeSH
• Publikační typ
• časopisecké články MeSH
• srovnávací studie MeSH
• Názvy látek
• antiinfekční látky MeSH
• cholesterol MeSH
• kvartérní amoniové sloučeniny MeSH
• terpeny MeSH

The resistance among microbes has brought an urgent need for new drugs. Thus, we synthesized a series of Schiff bases derived from the sulfa drug sulfadiazine and various salicylaldehydes. The resulting 4-[(2-hydroxybenzylidene)amino]-N-(pyrimidin-2-yl)benzene-sulfonamides were characterized and evaluated against Gram-positive and Gram-negative bacteria, yeasts, moulds, Mycobacterium tuberculosis, nontuberculous mycobacteria (M. kansasii, M. avium) and their cytotoxicity was determined. Among bacteria, the genus Staphylococcus, including methicillin-resistant S. aureus, showed the highest susceptibility, with minimum inhibitory concentration values from 7.81 µM. The growth of Candida sp. and Trichophyton interdigitale was inhibited at concentrations starting from 1.95 µM. 4-[(2,5-Dihydroxybenzylidene)amino]-N-(pyrimidin-2-yl)-benzenesulfonamide was identified as the most selective Schiff base for these strains with no apparent cytotoxicity and a selectivity index higher than 16. With respect to M. tuberculosis and M. kansasii that were inhibited within the range of 8 to 250 µM, unsubstituted 4-[(2-hydroxy-benzylidene)amino]-N-(pyrimidin-2-yl)benzenesulfonamide meets the selectivity requirement. In general, dihalogenation of the salicylic moiety improved the antibacterial and antifungal activity but also increased the cytotoxicity, especially with an increasing atomic mass. Some derivatives offer more advantageous properties than the parent sulfadiazine, thus constituting promising hits for further antimicrobial drug development.

• Klíčová slova
• Schiff bases, antibacterial activity, antifungal activity, antimycobacterial activity, cytotoxicity, sulfadiazine, sulfonamides,
• MeSH
• aldehydy chemická syntéza   farmakologie   MeSH
• antibakteriální látky chemická syntéza   chemie   farmakologie   MeSH
• antifungální látky chemická syntéza   chemie   farmakologie   MeSH
• antiinfekční látky chemická syntéza   farmakologie   MeSH
• buňky Hep G2 MeSH
• lidé MeSH
• mikrobiální testy citlivosti MeSH
• pyrimidiny chemická syntéza   farmakologie   MeSH
• Schiffovy báze chemická syntéza   farmakologie   MeSH
• sulfadiazin analogy a deriváty   chemická syntéza   farmakologie   MeSH
• viabilita buněk účinky léků   MeSH
• vztahy mezi strukturou a aktivitou MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• aldehydy MeSH
• antibakteriální látky MeSH
• antifungální látky MeSH
• antiinfekční látky MeSH
• pyrimidiny MeSH
• salicylaldehyde MeSH Prohlížeč
• Schiffovy báze MeSH
• sulfadiazin MeSH

Inspired by the high antituberculous activity of novel nitro-substituted derivatives and based on promising predicted ADMET properties we have synthesized a series of 33 salicylanilides containing nitro-group in their salicylic part and evaluated them for their in vitro antimycobacterial, antimicrobial and antifungal activities. The presence of nitro-group in position 4 of the salicylic acid was found to be beneficial and the resulting molecules exhibited minimum inhibitory concentrations (MICs) ranging from 2 to 32 μM against Mycobacterium tuberculosis. The best activity was found for 2-hydroxy-4-nitro-N-[4-(trifluoromethyl)phenyl]benzamide (MIC=2 μM). 4-Nitrosalicylanilides were also found to be active against all Staphylococcus species tested while for MRSA strain 2-hydroxy-4-nitro-N-[4-(trifluoromethyl)phenyl]benzamide's MIC was 0.98 μM. None of the nitrosalicylanilides was active against Enterococcus sp. J 14365/08 and no considerable activity was found against Gram-negative bacteria or fungi. The hepatotoxicity of all nitrosalicylanilides was found to be in the range of their MICs for HepG2 cells.

• Klíčová slova
• Cytotoxicity, In silico ADMET prediction, In vitro antimicrobial activity, In vitro antimycobacterial activity, Nitro group, Salicylanilides,
• MeSH
• antiinfekční látky chemická syntéza   farmakologie   toxicita   MeSH
• buňky Hep G2 MeSH
• Enterococcus účinky léků   MeSH
• houby účinky léků   MeSH
• lidé MeSH
• mikrobiální testy citlivosti MeSH
• Mycobacterium tuberculosis účinky léků   MeSH
• salicylanilidy chemie   farmakologie   MeSH
• salicylany chemická syntéza   chemie   farmakologie   toxicita   MeSH
• Staphylococcus účinky léků   MeSH
• viabilita buněk účinky léků   MeSH
• vztahy mezi strukturou a aktivitou MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• antiinfekční látky MeSH
• salicylanilidy MeSH
• salicylany MeSH

BACKGROUNDS: Snails (Gastropoda) have a mechanism for the production of a significant amount of slime and substances contained therein they use to protect themselves against bacterial or fungal pathogens. These active substances are involved in both humoral and cellular immune responses of the gastropods. The antibacterial or antifungal effect of the humoral immune component of slime lies in cytotoxic and haemagglutination activity against potential microbial pathogens. The activity of antibacterial agents present in Achatina reticulata slime against bacterial strains of Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae, and Pseudomonas aeruginosa was tested. MATERIAL AND METHODS: A total of five samples of slime from laboratory reared Achatina reticulata were tested. To eliminate potential microbial contamination, slime samples were sterilized by UV radiation. To screen slime samples for antibacterial activity, the simple diffusion method on Mueller-Hinton agar was used. Samples diluted in guaiacol glycerol ether were used in the testing. RESULTS: The results show that the biologically active substances present in Achatina reticulata slime have an antimicrobial activity which is almost commensurate with that of the conventional antibiotics used to treat bacterial infections. The results of the determination of the antimicrobial effects of Achatina reticulata slime also highlighted viridation (partial hemolysis of erythrocytes after 24 hours of slime cultivation exposed to UV light for 60 minutes on Columbia blood agar. CONCLUSIONS: The results of the antimicrobial activity testing of selected Achatina reticulata slime samples show that the gastropod slime contains biologically active substances with a relatively significant antimicrobial activity.

• Klíčová slova
• Achatina reticulata, antimicrobial activity of snail slime,
• MeSH
• antiinfekční látky * farmakologie   MeSH
• Bacteria * účinky léků   MeSH
• hlen mikrobiologie   MeSH
• mikrobiální testy citlivosti MeSH
• plži * mikrobiologie   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antiinfekční látky * MeSH

The antimicrobial activity of the protoberberine alkaloid, berberine, isolated from Mahonia aquifolium, was evaluated against 17 microorganisms including two Gram-negative bacteria--Pseudomonas aeruginosa and Escherichia coli (both resistant and sensitive), two Gram-positive bacteria--Bacillus subtilis and Staphylococcus aureus, Zoogloea ramigera, six filamentous fungi--Penicilium chrysogenum, Aspergillus niger, Aureobasidium pullulans (black and white strain), Trichoderma viride (original green strain and brown mutant), Fusarium nivale, Mycrosporum gypseum and two yeasts--Candida albicans and Saccharomyces cerevisiae. The IC50, minimum inhibitory concentration (MIC), minimum microbicidal concentration (MMC) and minimum microbistatic concentration (MMS) varied considerably depending on the microorganism tested, the sensitivity decreasing as follows: S. aureus > P. aeruginosa S (sensitive) > E. coli S > P. aeruginosa R (resistant) > E. coli R > B. subtilis > Z. ramigera > C. albicans > S. cerevisiae > A. pullulans B (black) > A. pullulans W (white) > T. viride Br (brown) > M. gypseum > A. niger > F. nivale > P. chrysogenum > T. viride G (green).

• MeSH
• antibakteriální látky MeSH
• antibiotická rezistence MeSH
• antifungální látky izolace a purifikace   farmakologie   MeSH
• antiinfekční látky izolace a purifikace   farmakologie   MeSH
• berberin izolace a purifikace   farmakologie   MeSH
• gramnegativní bakterie účinky léků   MeSH
• grampozitivní bakterie účinky léků   MeSH
• houby účinky léků   MeSH
• kvasinky účinky léků   MeSH
• Mahonia chemie   MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antibakteriální látky MeSH
• antifungální látky MeSH
• antiinfekční látky MeSH
• berberin MeSH