Showing papers on "Antibacterial activity published in 1995"
TL;DR: This investigation compared the antibacterial effects of amalgam, zinc oxide-eugenol, Super EBA and a mineral trioxide aggregate on nine facultative bacteria and nine strict anaerobic bacteria.
347 citations
TL;DR: An antibacterial peptide from bovine milk inhibiting the growth of Escherichia coli, and Staphylococcus carnosus is isolated and characterization by means of Edman amino acid sequencing and mass spectrometry.
194 citations
TL;DR: The results suggest that the N-terminal portion of the peptide, containing a predicted α-helix, is responsible for an increase in the membrane permeability, and proposes the name “moricin” for this novel antibacterial peptide isolated from B. mori.
186 citations
TL;DR: The amino acid sequences clearly show that the three peptides are novel isoforms of the insect defensin family of antibacterial peptides, which are potently active against Gram-positive bacteria and against one of the Gram-negative bacteria that were tested.
146 citations
TL;DR: Three structurally related and novel antibacterial peptides have been isolated from the haemolymph of the silkworm, Bombyx mori, immunized with Escherichia coli, and the name 'lebocin' is proposed for the novel peptide family isolated from B. mori.
Abstract: Three structurally related and novel antibacterial peptides have been isolated from the haemolymph of the silkworm, Bombyx mori, immunized with Escherichia coli. These peptides were 32 amino acids long and characteristically rich in proline residues. A unique threonine residue in each peptide was O-glycosylated and the modification seemed to be important for expression of antibacterial activity. The primary structure and antibacterial character of the novel peptides resemble those of abaecin (41% identity in amino acid sequence), an antibacterial peptide of the honeybee, although abaecin is not O-glycosylated. Incubation of the novel peptides with a liposome preparation caused leakage of entrapped glucose under low-ionic-strength conditions, suggesting that a target of the peptides is the bacterial membrane. We propose the name 'lebocin' for the novel peptide family isolated from B. mori.
139 citations
TL;DR: These extracts were found to be non-cytotoxic and effective antibacterial agents and studied against dysentery causing Shigella spp.
124 citations
TL;DR: The antibacterial activity of extracts from Helichrysum aureonitens was investigated and the dichloromethane extract was active against all five gram positive bacteria tested and the methanol Extract was active only against Bacillus cereus, B. pumilus and Micrococcus kristinae.
120 citations
TL;DR: Some 68 plant extracts from 65 species belonging to 25 families were investigated for antibacterial activity against eight gram‐positive and gram‐negative bacteria and among the active extracts, 12 from 11 species exhibited a broad spectrum of activity.
Abstract: Some 68 plant extracts from 65 species belonging to 25 families were investigated for antibacterial activity against eight gram-positive and gram-negative bacteria. Of the 68 extracts, 64 (94.1%) exhibited inhibitory effects against one or more microorganisms. Furthermore, among the active extracts, 12 from 11 species exhibited a broad spectrum of activity. Discussion on the probable chemical components responsible for this activity is included.
114 citations
TL;DR: These derivative compounds possess antibacterial activity against a wide variety of bacteria, including activity against vancomycin-resistant isolates.
81 citations
TL;DR: The series of 8-methoxyquinolones had antibacterial activity against Gram-positive, Gram-negative, and anaerobic bacteria equivalent to the most active 8-substituted compounds (8-F and 8-Cl) and a concomitant reduction in several of the potential side effects.
Abstract: A series of 1-cyclopropyl-6-fluoro-8-alkoxy (8-methyoxy and 8-ethoxy)-quionoline-3-carboxylic acids and 1-cyclopropyl-5-amino-6-fluoro-8-alkoxyquinoline-3-carboxylic acids has been prepared and evaluated for antibacterial activity. In addition, they were also compared to quinolones with classic substitution at C8 (H, F, Cl) and the naphthyridine nucleus in a phototoxicity and mammalian cell cytotoxicity assay. The series of 8-methoxyquinolones had antibacterial activity against Gram-positive, Gram-negative, and anaerobic bacteria equivalent to the most active 8-substituted compounds (8-F and 8-Cl). There was also a concomitant reduction in several of the potential side effects (i.e., phototoxicity and clonogenicity) compared to the most active quinolones with classic substitution at C-8. The 8-ethoxy derivatives had an even better safety profile but were significantly less active (2-3 dilutions) in the antibacterial assay.
65 citations
TL;DR: The morphological effect of disinfectants in aqueous solution on the antibacterial activity is discussed for low molecular weight phosphonium salts with single and double long alkyl chains (carbon number 14).
Abstract: A new concept for the mode of action of cationic biocides is proposed in which the antibacterial activity of cationic disinfectants is ascribed essentially to molecular organizations of cations within aggregates, i.e. the activity is determined by the size of aggregates and number of active molecules comprising the aggregate. On the basis of the new concept, the morphological effect of disinfectants in aqueous solution on the antibacterial activity is discussed for low molecular weight phosphonium salts with single and double long alkyl chains (carbon number 14). The proposed new concept can be applied to all phenomena reported previously in antibacterial activity of cationic biocides and this concept is very important from the viewpoint of molecular design of more active cationic biocides.
TL;DR: The purification of antibacterial protein was found to have comparable antibacterial activity against both E. coli and Micrococcus luteus and the antibacterial properties of the purified protein were found to be partially heat labile.
TL;DR: The antibacterial activity of AM-1155 was almost equal to that of sparfloxacin against a wide range of Gram-positive and Gram-negative species and showed a good activity against anaerobes.
Abstract: AM-1155 is a new 8-methoxy quinolonecarboxylic acid with a broad spectrum of antibacterial activity. It inhibited more than 90% of clinical isolates of methicillin-susceptible Staphylococcus aureus, streptococci, Enterococcus faecalis, most of the Enterobacteriaceae, Acinetobacter calcoaceticus and Haemophilus influenzae at the concentration of 0.39 mg/L. AM-1155 was 2- to 16-fold more active than ciprofloxacin against Gram-positive organisms including methicillin-resistant staphylococci. The antibacterial activity of AM-1155 was almost equal to that of sparfloxacin against a wide range of Gram-positive and Gram-negative species. AM-1155 also showed a good activity against anaerobes. The protective efficacy of AM-1155 against experimental systemic infections with Gram-positive and Gram-negative pathogens in mice was almost equal or superior to that of sparfloxacin. AM-1155 was 5- to 28-times more effective than ciprofloxacin, in terms of ED50 at one week, in staphylococcal and streptococcal infections.
Journal Article•
TL;DR: The influence of the genetic background of a plant on the antibacterial activity of essential oil derived from it was investigated andinterspecific and intra-specific differences were evident in the antib bacterial activity of the essential oils derived from the the six Cymbopogon strains.
Abstract: The influence of the genetic background of a plant on the antibacterial activity of essential oil derived from it was investigated. Essential oils from six distinct strains of Cymbopogon were tested against eighteen bacteria. Interspecific and intra-specific differences were evident in the antibacterial activity of the essential oils derived from the the six Cymbopogon strains.
TL;DR: The synthesis and antimicrobial activity of new N -heteroaryl benzylamines and their Schiff bases are reported and some of the tested compounds possessed moderate activity against strains of Candida albicans, Candida sp and good activity against isolates of plant pathogenic fungi.
Patent•
14 Jun 1995
TL;DR: In this paper, a quinoline(naphthyridine)carboxylic acid derivative represented by the following formula (I) has an 4-aminomethyl-3-oximepyrrolidine substituent on 7-position of the quinolone nucleus and shows a superior antibacterial activity in contrast to the known quinolate antibactrial agents having a weak activity against gram-positive bacterial strains and also has a broad antibacterial spectrum and a highly improved pharmacokinetic property.
Abstract: The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to a novel quinoline(naphthyridine)carboxylic acid derivative represented by the following formula (I), which has an 4-aminomethyl-3-oximepyrrolidine substituent on 7-position of the quinolone nucleus and shows a superior antibacterial activity in contrast to the known quinolone antibactrial agents having a weak activity against gram-positive bacterial strains and also has a broad antibacterial spectrum and a highly improved pharmacokinetic property : wherein R, R₁, R₂, R₃, R₄ and Q are defined as described in the specification.
TL;DR: The palladium-catalyzed coupling of 3- and 4-(trialkylstannyl)pyridines with 7-bromo or 7-chloro 1-substituted 1,4-dihydro-4-oxo-7- pyridinyl-3-quinolinecarboxylic acid derivatives provided equal antibacterial activity against Staphylococcus aureus ATCC 29213.
Abstract: The palladium-catalyzed coupling of 3- and 4-(trialkylstannyl)pyridines with 7-bromo or 7-chloro 1-substituted 1,4-dihydro-4-oxo-3-quinolinecarboxylates has provided access to the corresponding 1-substituted 1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids. The antibacterial activity of these derivatives was studied with the finding that the optimal 1- and 7-position substituents for Gram positive activity are cyclopropyl and 4-(2,6-dimethylpyridinyl), respectively. We find that for the fluorine-substituted derivatives studied, the position of the fluorine on the quinolone nucleus or the number of fluorine atoms does not seem to be important for good Gram positive activity. For 1-cyclopropyl 7-(2,6-dimethyl-4-pyridinyl) derivatives, the 6-fluoro 4a, 8-fluoro 10d, 6,8-difluoro 10b, and 5,6,8-trifluoro 8, all provided equal antibacterial activity against Staphylococcus aureus ATCC 29213. There is also a correlation between the substitution on the 7-(4-pyridinyl) group and the Gram positive activity, particularly for S. aureus, clearly indicating that the 2,6-dimethylpyridinyl group is optimal. The MIC50 value for the most potent agents in this study against S. aureus ATCC 29213 is 0.008 microgram/mL. By comparison, ciprofloxacin and aminopyrrolidine 28 gave values of 0.25 and 0.015 microgram/mL, respectively, against this organism.
TL;DR: The methyl phosphonates in general were stable to a wide range of beta-lactamases, including the TEM enzymes and the Enterobacter cloacae P99 chromosomal enzyme, and showed the advantage of being highly water soluble.
Abstract: A series of cephalosporins containing a novel 7-[2-(Z)-(2-amino-thiazol-4-yl)-3-(dimethoxyphosphoryl)-acryloylamino] group were prepared and their antibacterial activity measured against a range of pathogens. In general the compounds displayed a broad spectrum of activity against both Gram positive and Gram negative organisms, except Pseudomonas aeruginosa. Activity against the latter could be achieved by introducing a catechol moiety at the 3 position of the cephalosporin. The methyl phosphonates in general were stable to a wide range of β-Mactamases, including the TEM enzymes and the Enterobacter cloacae P99 chromosomal enzyme. In addition, they showed the advantage of being highly water soluble.
TL;DR: Structural-activity relationship studies indicated that the absolute stereochemistry at the asymmetric centers of both the azetidine and the oxazine rings was critical to increase in vitro activity and oral efficacy.
Abstract: A series of stereochemically pure 7-(3-amino-2-methyl-1-azetidinyl)-1,4- dihydro-6-fluoro-4-oxoquinoline- and -1,8-naphthyridine-3-carboxylic acids, with varied substituents at the 1-, 5-, and 8-positions, was prepared to determine the effects of chirality on potency and in vivo efficacy relative to the racemic mixtures (for part 2, see: J. Med. Chem. 1994, 37, 4195-4210). A series of chiral 9-fluoro-2,3-dihydro-3-methyl-7-oxo-10-(substituted-1- azetidinyl)-7H-pyrido[1,2,3- de]-1,4-benzoxazine-6-carboxylic acids was synthesized to study the effect of the azetidine moiety on tricyclic quinolone antibacterial agents. A series of amino acid prodrugs of chiral naphthyridines 24a and 24b and quinolone 33a (cetefloxacin) was prepared and evaluated for antibacterial activity, solubility, and pharmacokinetic behavior. The absolute configuration of the new azetidinylquinolones was established by X-ray analysis of one of the diastereomeric salts of the resolved azetidinols (15) and of compound 25a (E-4767), which showed the best in vitro and in vivo overall profile. Structure-activity relationship studies indicated that the absolute stereochemistry at the asymmetric centers of both the azetidine and the oxazine rings was critical to increase in vitro activity and oral efficacy. The 3S configuration in the pyridobenzoxazine series and the (2S,3R) configuration of the 3-amino-2-methylazetidine moiety for all new compounds conferred the best antibacterial activity.
Patent•
15 Jun 1995
TL;DR: In this article, a quinoline(naphthyridine)carboxylic acid derivative represented by the following formula (I), which has an 4-aminomethyl-3-oximepyrrolidine substituent on 7-position of the quinolone nucleus and shows a superior antibacterial activity in contrast to the known quinolate antibacterial agents having a weak activity against gram-positive bacterial strains and also has a broad antibacterial spectrum and a highly improved pharmacokinetic property.
Abstract: The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to a novel quinoline(naphthyridine)carboxylic acid derivative represented by the following formula (I), which has an 4-aminomethyl-3-oximepyrrolidine substituent on 7-position of the quinolone nucleus and shows a superior antibacterial activity in contrast to the known quinolone antibacterial agents having a weak activity against gram-positive bacterial strains and also has a broad antibacterial spectrum and a highly improved pharmacokinetic property: ##STR1## wherein R, R 1 , R 2 , R 3 , R 4 and Q are defined as described in the specification.
TL;DR: Since compound 12 exhibits good activity, in order to clarify the effect of substituents at C‐1 on the activity, benzimidazole derivatives having ethyl, allyl, benzyl, and p‐fluorobenzyl substituency were prepared, and slightly increased activity was seen.
Abstract: A series of 22 benzimidazoles, having several substituents on the azole and benzene nuclei, were prepared and evaluated in vitro for antimicrobial activity. At first 2-chloro or 2-chloromethyl-5(6)-substituted-1H-benzimidazoles were synthesized, which were then substituted at C-2 with several piperazine or piperidine derivatives. The antibacterial activity of these compounds against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa, and the antifungal activity against Candida albicans, Candida stellatoidea, Candida parapsilosis, and Candida pseudotropicalis were determined as the MIC values. Since compound 12 exhibits good activity, in order to clarify the effect of substituents at C-1 on the activity, benzimidazole derivatives having ethyl, allyl, benzyl, and p-fluorobenzyl substituents at C-1 were prepared, and slightly increased activity was seen.
TL;DR: A series of 2-carbolinyl-carbapenems was prepared via the Stille stannane coupling reaction and exhibited potent activity in vitro against methicillin-resistant Staphylococcus aureus, MRSA and MRCNS as well as a broad spectrum of antibacterial activity.
Patent•
29 Aug 1995
TL;DR: In this article, a peptide represented by the amino acid sequence of SEQ ID NO: 1, an antibacterial agent comprising the peptide as an active ingredient, peptide gene encoding peptide, a recombinant DNA comprising peptide genes and a method for producing peptide was presented.
Abstract: The present invention relates to a peptide represented by the amino acid sequence of SEQ ID NO: 1, an antibacterial agent comprising the peptide as an active ingredient, a peptide gene encoding the peptide, a recombinant DNA comprising the peptide gene and a method for producing a peptide. The peptide of the present invention exhibits an effective antibacterial activity against various Gram-negative and -positive bacteria including Staphylococcus aureus and Bacillus cereus which are pathogenic bacteria causing food poisoning. Therefore, this peptide is useful as a food preservative and an antibacterial agent for medical use.
Journal Article•
TL;DR: In this article, the synthesis of 15 new N-benzyl substituted derivatives of (E)-gamma-azastilbenols and their antimicrobial activity was reported.
Abstract: The synthesis of 15 new N-benzyl substituted derivatives of (E)-gamma-azastilbenols-2'(3' and 4') and their antimicrobial activity are reported. In particular, compounds 1a-c, 1h and 2a-b showed good antibacterial activity against Staphlococcus aureus.
TL;DR: The crude ethanol extract from the leaves of Tovomitopsis psychotriifolia exhibits antibacterial activity against Bacillus cereus, Staphylococcus aureus, and Pseudomonas aeruginosa.
Abstract: The crude ethanol extract from the leaves of Tovomitopsis psychotriifolia (Clusiaceae) exhibits antibacterial activity against Bacillus cereus, Staphylococcus aureus, and Pseudomonas aeruginosa. The biologically active agent in the extract has been isolated by chromatographic techniques and identified by NMR spectroscopy as trans-delta-tocotrienoloic acid.
TL;DR: In this paper, 4-(cyclic amino)-5-fluoro-imidazoquinolones 31 a-d showed potent and well balanced antibacterial activity against both gram-positive and gram-negative bacteria.
Abstract: 4,5-Disubstituted 6-cyclopropyl-6,9-dihydro-9-oxo-1H-imidazo (30-32) and triazolo[4,5-f]quinoline-8-carboxylic acids (33-35) were synthesized starting from 5,6-diaminoquinolones 25. The imidazoquinolones 30-32 were equal or superior to the corresponding triazoloquinolone analogues 33-35 in in vitro antibacterial activity. As for the C-5 substituents, a fluorine atom was the most favorable of the three groups, H, F, and Cl. Among the compounds prepared, 4-(cyclic amino)-5-fluoro-imidazoquinolones 31 a-d showed potent and well-balanced antibacterial activity against both gram-positive and gram-negative bacteria. Structure-activity relationships for the C-4 substituents (cyclic amino groups) were also examined in detail.
TL;DR: The derivatives of tetrodecamycin, being introduced acyl, carbamoyl and alkyl groups at 14-hydroxyl group and modified at exo-methylene group, were synthesized and evaluated on their antibacterial activities.
Abstract: The derivatives of tetrodecamycin (1), being introduced acyl, carbamoyl and alkyl groups at 14-hydroxyl group and modified at exo-methylene group, were synthesized and evaluated on their antibacterial activities. Although 14-O-substituted tetrodecamycins (3 approximately 19) showed weak activity against Pasteurella piscicida, they were more active against Gram-positive bacteria than 1. Among them, 15 showed approximately 10-fold higher activity than 1. The derivatives (20 approximately 23) modified at 4 or 5 positions had moderate antibacterial activity. The absolute structure of 4(R),5-dibromotetrodecamycin (23) was determined by X-ray crystallographic analysis.
TL;DR: In this article, a series of 9a- N-N′ -substituted carbamoyl and thiocarbamoyal derivatives of 9-deoxo-9a-aza-ninea-homoerythromycin A was synthesized and structurally characterized by spectroscopic methods and X-ray crystallographic analysis.
TL;DR: The authors showed no antibacterial activity against Bacillus subtilis, Escherichia coli, P. coli, and Bacillia coli using 4-arylthiosemicarbazides and 6-thioxo-1,2,4-triazol-3yl.