Antibacterial and Antifungal Activity of Zinc(II) Carboxylates With/Without N-Donor Organic Ligands.

The antibacterial and antifungal activity of zinc(II) carboxylates with composition Zn(RCOO)(2)*nH(2)O(R =H-, CH(3) (-), CH(3)CH(2)CH(2) (-), (CH(3))(2)CH-, XCH(2) (-), X=Cl, Br, I, n=0 or 2), [ZnX(2)(Nia(+)CH(2)COO(-))(2)](Nia=nicotinamide, X=Cl, Br, I) and [Zn(XCH(2)COO)(2)(Caf)(2)]*2H(2)O (Car=caffeine, X=Cl, Br) is studied against bacterial strains Staphylococcus aureus, Escherichia coli and yeast Candida albicans. The structural types are assigned to the prepared compounds and the influence of (i) carboxylate chain length, (ii) substitution of hydrogen atom of carboxylate by halogen and (iii) presence of N-donor organic ligands on the biological activity is discussed.

Effects of LPS, lipid A and polysaccharide from adapted strains of Escherichia coli on human leucocyte activity.

Polysaccharide and lipid A are responsible for the wide-ranging pharmacological activity of bacterial lipopolysaccharides (LPS). The alterations in LPS structure result in various effects on different functions of the target cells. The effects of LPS substructures, the polysaccharide (P) and lipid A (L) from E.

Activation of human leukocytes by lipid A from E. coli strains adapted to quaternary ammonium salt and amine oxide.

The immunomodulatory activities of monophosphoryl lipid A (MLA) and diphosphoryl lipid A analogues obtained from the sensitive strain of E. coli and from the resistant strains adapted to a quaternary ammonium salt and an amine oxide were compared. All analogues considerably stimulated the activity of human leukocytes although the analogue from the sensitive strain at a higher concentration significantly suppressed phagocytosis.

[Antimicrobial activity of (N-salicylidene-DL-aspartate- and (N-salicylidene-L-asparaginate)-copper complexes with pyrazole-type ligands].

By a reaction of salicylaldehyde (Scl) with the corresponding amino acids and by the next complexation reaction of the formed Schiff bases with Cu2+ ions in an aqueous-alcoholic medium, aqua (N-salicylideneaminoalkanoato)copper(II) complex chelates of the composition Cu(Scl-DL-Asp(2-)) (H2O)2, Ip and Cu(Scl-L-Asn(2-)(H2O), In were prepared. The monodiazole complexes with pyrazole IIp and IIn (as monohydrate) as well as with 3,5-dimethylpyrazole IIIp a IIIn were prepared by replacing the molecule of H2O in the parent aquacomplexes with the diazoles under the same reaction conditions. Using a routine dilution micromethod, the antimicrobial activity of the prepared complexes and free diazoles was tested against Staphylococcus aureus, Escherichia coli and Candida albicans.

Transduction of antibiotic resistance including imipenem resistance by wild type phages from nosocomial strains of Pseudomonas aeruginosa.

In this report we describe transduction of antibiotic resistance determinants by three wild type bacteriophages isolated from three Pseudomonas aeruginosa strains. The strains showed evident plaques of a lysis caused by a bacteriophage. The strains were identified as lysogenic among 31 imipenem (IMP)-resistant P.

Stereoisomeric effect on antimicrobial activity of a series of quaternary ammonium salts.

Two homologous series of diastereoisomeric racemic +/- cis and +/- trans-N,N-dimethyl-N-alkyl-2-benzoyloxycyclohexylmethylammonium bromides with the number of carbon atoms in the alkyl chain from six to twenty (m = 6,8 ...

Immunomodulatory activity of amphiphilic antimicrobials on mouse macrophages.

A quaternary ammonium salt (1-methyldodecyl)-trimethylammonium iodide, a structurally analogous amine oxide (1-methyldodecyl)-dimethylamine-N-oxide and the amine oxide lacking long alkyl chain trimethylamine-N-oxide were tested for their immunomodulatory activity. Inbred mice strain C57/BL6 were pretreated for 7 days by the compounds under study. The activity of elicited peritoneal macrophages was also tested.

Suppression of virulence factors of pseudomonas aeruginosa by subinhibitory concentrations of quaternary ammonium salts.

The effect of subinhibitory concentrations (sub-MICs) of two homologous series of "soft" quaternary ammonium salts (QATs) upon the expression of phospholipase C (Pseudomonas aeruginosa strain 72/92), elastase, proteinase and permeability activity (P. aeruginosa 9/92) was studied. Both strains were isolated from the patients suffering from nosocomial infections.

Efficacy of new organic ammonium salts on Pseudomonas aeruginosa Salmonella typhimurium.

The inhibitory activities of four new homologous series of organic ammonium salts (OAS) were tested on bacterial strains isolated from patients. Two types of compounds are used: "hard" (group A) and three groups (B, C, D) of biodegradable "soft" OAS with metabolically labile CO or NH groups in their molecules. The strain Pseudomonas aeruginosa was isolated from the sputum of a patient with carcinoma.

Effect of quaternary ammonium salts and amine oxides on Pseudomonas aeruginosa.

Two quaternary ammonium salts, viz (1-methyldodecyl) trimethylammonium bromide (ATDBr) and tetramethylammonium bromide (TMABr), as well as two amine oxides, (1-methyldodecyl)dimethylamine oxide (ATDNO) and trimethylamine oxide (TMANO), were tested for their inhibitory activity on a Pseudomonas aeruginosa strain isolated from nosocomial infections. Only those compounds with long alkyl chains in their molecules (ATDBr and ATDNO) showed antimicrobial efficacy. In subinhibitory concentrations both compounds inhibited incorporation of [14C]-adenine and [14C]-leucine as precursors of macromolecular biosynthesis.

[Antimicrobial activity of diazole-(N-salicylidene-L-alpha- alaninato)-copper complexes].

The antimicrobial activities of a group of copper(II) chelates with the composition [Cu(TSB)(L)] or [Cu(TSB)(L')]. (TSB = N-salicylidene-L-alpha-alaninate dianion, L = imidazole and its alkyl derivatives, L' = pyrazole and 3,5-dimethylpyrazole) were studied. Bis-diazole complexes with L' = pyrazole and 3,5-dimethylpyrazole were found to be the most active against S.

Primary biodegradation of amine oxide and quaternary ammonium amphiphiles.

Biodegradation of two amphiphilic "soft" antimicrobially active derivatives of lauric (dodecanoic) acid, a quaternary ammonium salt and an amine oxide bearing an amide or ester group, was followed using microorganisms from activated sludge. Primary biodegradation was determined by ion-selective electrodes, total biodegradation as the chemical oxygen demand. Though organic ammonium salts quickly undergo primary biodegradation, the rest of the molecule is difficult to destroy.

[Immunochemical changes in the outer membrane of Escherichia coli adapted to amine oxides].

Resistant strains of Escherichia coli were obtained by stepwise cultivation in subinhibitory concentrations of two antimicrobially active amine oxides. Changes in the chemical composition of the outer membrane of the resistant strains were accompanied also by different antigenic reactions. New precipitation lines were revealed by double immunodiffusion and immuno-electrophoretic methods.

[Antimicrobial activity of selected aqua-carboxyl-cupric complexes].

The activity of compounds of different structural types of aqua-complexes of the composition Cu(R-COO)2.nH2O-methoxybenzoatocupric complexes, R = 2-, 3- and 4-methoxyphenyl (n = 1, 1 and 3); aryloxyacetatocupric complexes, R = phenoxymethyl (n = 3), 2-, 3- and 4-chlorophenoxymethyl (n = 4, 2 and 2) and 1-naphthoxymethyl (n = 4), and furthermore isomeric furanecarboxylato-(R = 2- or 3-furyl, n = 3, or 1) and thiophencarboxylatocupric complexes (R = 2- or 3-thienyl, n = 1 and 1), was examined by the methods of the 1st screening on selected anthropo- and phytopathogenic microorganisms. The effects of all aqua-complexes (suspension dosage form) on the representatives of bacteria and yeasts are minimal.

Potassium leakage from Escherichia coli cells treated by organic ammonium salts.

The effect of the homologous series of 1,1-dialkylpiperidinium bromides on the potassium leakage from Escherichia coli cells has been studied. The minimum concentration for each compound which is able to release maximum of cellular potassium has been determined and correlated with the inhibitory activities of the compounds. The relationship between the structure and the activity enables to consider the K+ leakage as the marker of inhibitory activity of the membrane active antimicrobials.

Enhanced biodegradation of a hard bis-quaternary ammonium salt.

Bacterial strains with a high biodegradation potential were isolated from activated sludge. Their ability to decompose the hard bis-quaternary ammonium salt FB was determined by the method of chemical oxygen demand (COD) in a mineral medium, where the compound FB was the only source of carbon. The COD values were very low after 21 d and in the course of this period they reached zero level twice.

[The effect of piperidinoethylesters of n-alkoxyphenyl-carbamic acids on bacterial cells].

The inhibitory effect of local anaesthetic agents of this type on the bacteria Escherichia coli were evaluated. The dependence between antimicrobial activity and structure (log 1/MIC = f/m) was studied with the use of a bilinear model. In the positional paraisomers a lower effect of spherical and electron effects than in the case of ortho- and meta-isomers is assumed.

Adsorption on bacterial spores depending on the aggregation properties of antimicrobial tensides.

A change in interaction with spores of Bacillus cereus occurred in the range of critical concentrations of micelle formation. With 1-methyldodecyldimethylamine-N-oxide and N,N'-bis(dodecyldimethyl)-1,2-ethanediammonium dibromide, the induced release of dipicolinic acid was blocked and the adsorption dynamics changed, respectively.

Interaction of amine oxides and quaternary ammonium salts with membrane and membrane-associated processes in E. coli cells: mode of action.

The antimicrobials (1-methyldodecyl)dimethylamine oxide and (1-methyldodecyl)trimethylammonium bromide affect the cytoplasmic membrane of E. coli. The interaction results in release of intracellular material (K+, 260nm-absorbing material), an effect on dehydrogenase enzyme activity and inhibition of respiration.

Inhibitory effect of 1-methyldodecyldimethylamine oxide and N,N-bis(dodecyldimethyl)-1,2-ethanediammonium dibromide on the spores of Bacillus cereus.

1-Methyldodecyldimethylamine oxide (MDDO) and N,N'-bis(dodecyldimethyl)-1,2-ethanediammonium dibromide (BDED) exhibit a significant affinity for the surface of Bacillus cereus spores and adsorb very rapidly to the cells; they have a pronounced inhibitory effect on spore outgrowth. In order to alter the affinity of the spore surface for these inhibitors, the spores were pretreated with sodium dodecyl sulfate (SDS), and with an electronegative (Tween 80) and electropositive (histone) compound. In SDS-pretreated spores the inhibitory effect of MDDO and BDED was abolished to a considerable extent.