scholarly journals Synthesis, Characterization and Antimicrobial Activity of Imidazole Derivatives Based on 2-chloro-7-methyl-3-formylquinoline

2012 ◽  
Vol 9 (3) ◽  
pp. 1188-1195 ◽  
Author(s):  
R. H. Parab ◽  
B. C. Dixit
Keyword(s):  
Antimicrobial Activity ◽  
Biological Activity ◽  
Bacterial Species ◽  
Gram Positive ◽  
Gram Negative ◽  
Imidazole Derivatives

A series of oxazole and thereof imidazole derivatives were prepared from 2-chloro-7-methyl-3-formyl quinoline. The structures of all synthesized compounds were elucidated by elemental, IR,1HNMR,13CNMR spectra. Supplementary to these, they were assayedin vitrofor their antimicrobial activity; it was revealed that some synthesized derivatives were exhibiting competent biological activity against both gram negative and gram positive bacterial species and fungal microorganisms.

Biosynthesis of Silver Nanoparticles by Punica Granatum Peel Extract and their Biological Activity on different Pathogenic Bacteria

2021 ◽  
Vol 19 (9) ◽  
pp. 38-45
Author(s):  
Hussein H. Al-Turnachy ◽  
Fadhilk. alibraheemi ◽  
Ahmed Abd Alreda Madhloom ◽  
Zahraa Yosif Motaweq ◽  
Nibras Yahya Abdulla
Keyword(s):  
Antimicrobial Activity ◽  
Silver Nanoparticles ◽  
Biological Activity ◽  
Pathogenic Bacteria ◽  
Punica Granatum ◽  
Gram Positive ◽  
Gram Negative ◽  
Inhibition Zones ◽  
Peel Extract

The present study was included the assessment of the antimicrobial activity of AgNPs synthesized by Punica granatum peel extract against pathogenic bacteria by testing warm aqueous P. granatum peel extract and silver nanoparticles. Punica granatum indicated potency for AgNP extracellular nanobiosynthesis after addition of silver nitrate (AgNO3) 4mM to the extract supernatant, in both concentrations (100mg and 50mg). The biogenic AgNPs showed potency to inhibit both gram-negative and gram-positive bacterial growth. Zons of inhibition in (mm) was lesser in gram-positive than gram-negative bacteria. The resulted phytogenic AgNPs gave higher biological activity than warm aqueous Punica granatum peel extract. The inhibition zone of the phytogenic AgNPs on E. coli reached 17.53, 22.35, and 26.06 mm at (0.1, 0.5, and 1) mg/ml respectively. While inhibition zones of Punica warm aqueous extract reached 5.33, 10.63, and 16.08 mm at the same concentrations. phytogenic AgNPs gave smaller inhibition zones in gram-positive than gram- negative. Cytotoxic activity of the phytogenic AgNPs was assayed in vitro agaist human blood erythrocytes (RBCs), spectroscopic results showed absorbance at 540 nm hemolysis was observed. In general, AgNPs showed least RBCs hemolysis percentage, at 1 mg/ml concentration, hemolysis percentage was (4.50%). This study, concluded that the Punica granatum peel extract has the power of synthses of AgNPs characterized by broad spectrum antimicrobial activity with cyto-toxicity proportional to AgNPs concentration.

scholarly journals The antimicrobial activity of leaves and callus extracts of Thevetia peruviana In vitro

2013 ◽  
Vol 7 (3) ◽  
pp. 74-80
Author(s):  
Salah K. M. Alhashimi ◽  
Khaleel I. Rashid ◽  
Ghoson S. Saleh ◽  
Alea M. Abdulhadi ◽  
Tara A. Taher
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Leaf Extract ◽  
Bacterial Species ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Thevetia Peruviana

The antimicrobial activity for Thevietia peruviana was evaluated by measuring inhibition zone diameter in agar using well diffusion assay. The aim of the present study was to evaluate the antimicrobial potential of Thevietia peruviana leaf extract as compared with callus extract against some bacterial strains and fungi. The results showed that the addition of 2,4-D at the concentration of 9 mg/l, and 0.1 mg/l of kinetin led to obtain callus weight reached 800 mg. It was noticed that the reduction of 2,4-D concentration up to 6 mg/l resulted in compact and green pieces of callus. The optimal weight and friable callus was obtained at 9 mg/l. Among the susceptible bacteria are the gram negative pseudomonas aeruginosa seemed to be sensitive against all concentration of Thevietia peruviana leaf and callus extracts, While Escherichia coli showed resistance with all concentrations of extracts. It was noted that the extracts were more active against gram positive staphylococcus aureus, as compared with other bacterial species. Results of this study revealed that callus extract of Thevetia peruviana possess higher activity in comparison with leaf extract against gram positive bacteria (Staphylococcus aureus, Bacillus cereus) and gram negative (Pseudomonas aeruginosa). Finally all the bioextracts were well stable at room temperature during the period of the study and did not show any reduction of activity against the bacterial strains used in this study experiments.

scholarly journals PHYTOCHEMICAL INVESTIGATION AND IN VITRO ANTIMICROBIAL SCREENING OF SANTALUM ALBUM SEEDS EXTRACTS

2017 ◽  
Vol 9 (10) ◽  
pp. 117
Author(s):  
Gautam P. Vadnere ◽  
Md. Rageeb Usman ◽  
Santram Lodhi ◽  
Vaishali Patil
Keyword(s):  
Antimicrobial Activity ◽  
Petroleum Ether ◽  
Petroleum Ether Extract ◽  
Santalum Album ◽  
Ether Extract ◽  
Gram Positive ◽  
Gram Negative ◽  
Antimicrobial Screening ◽  
Ethanol Extracts

Objective: Present study aimed phytochemical evaluation and antimicrobial screening of petroleum ether and ethanol extracts of Santalum album seeds.Methods: Petroleum ether and ethanol extracts were screened for presence of chemical constituents. Petroleum ether extract was investigated detail by using chromatographic and spectroscopic methods. In vitro antimicrobial activity of both extracts were investigated using disc diffusion method on two gram-positive bacteria, Bacillus subtilis, Staphylococcus aureus, gram negative Pseudomonas aeruginosa, Escherichia coli and fungus Candida albicans.Results: Santalbic acid was identified in petroleum ether extract and content determined by HPTLC was 4.7%w/w. It was seen that petroleum ether extract have MIC value for B. subtilis, P. aeruginosa, E. coli and C. albicans were 78.125 µg/ml, 19.331 µg/ml, 625 µg/ml & 39.062 µg/ml respectively while MBC was 39.062 µg/ml, 4.882 µg/ml, 312.5 µg/ml & 9.765 µg/ml,  respectively. Petroleum ether extract showed MIC and MBC values for S. aureus was similar as 156.25µg/ml. So, the petroleum ether extract showed significant antimicrobial activity against both gram positive, gram negative and fungal strain.Conclusions: The results of present investigations were indicative of possible high potency of petroleum ether extract due to santalbic acid which could serve as chemotherapeutic agent.

scholarly journals In Vitro Study of Antimicrobial Percutaneous Nephrostomy Catheters for Prevention of Renal Infections

2017 ◽  
Vol 61 (6) ◽  
Author(s):  
Nylev Vargas-Cruz ◽  
Ruth A. Reitzel ◽  
Joel Rosenblatt ◽  
Mohamed Jamal ◽  
Ariel D. Szvalb ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biofilm Formation ◽  
In Vitro Study ◽  
Percutaneous Nephrostomy ◽  
Multidrug Resistant ◽  
Gram Positive ◽  
Gram Negative ◽  
Content Type ◽  
Fungal Organisms

ABSTRACT Percutaneous nephrostomy (PCN) catheters are the primary method for draining ureters obstructed by malignancy and preventing a decline of renal function. However, PCN catheter-related infections, such as pyelonephritis and urosepsis, remain a significant concern. Currently, no antimicrobial PCN catheters are available for preventing infection complications. Vascular catheters impregnated with minocycline-rifampin (M/R) and M/R with chlorhexidine coating (M/R plus CHD) have previously demonstrated antimicrobial activity. Therefore, in this study, we examined whether these combinations could be applied to PCN catheters and effectively inhibit biofilm formation by common uropathogens. An in vitro biofilm colonization model was used to assess the antimicrobial efficacy of M/R and M/R-plus-CHD PCN catheters against nine common multidrug-resistant Gram-positive and Gram-negative uropathogens as well as Candida glabrata and Candida albicans. Experimental catheters were also assessed for durability of antimicrobial activity for up 3 weeks. PCN catheters coated with M/R plus CHD completely inhibited biofilm formation for up to 3 weeks for all the organisms tested. The reduction in colonization compared to uncoated PCN catheters was significant for all Gram-positive, Gram-negative, and fungal organisms (P < 0.05). M/R-plus-CHD PCN catheters also produced significant reductions in biofilm colonization relative to M/R PCN catheters for Enterobacter spp., Escherichia coli, Pseudomonas aeruginosa, methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci, C. glabrata, and C. albicans (P < 0.05). M/R-plus-CHD PCN catheters proved to be highly efficacious in preventing biofilm colonization when exposed to multidrug-resistant pathogens common in PCN catheter-associated pyelonephritis. M/R-plus-CHD PCN catheters warrant evaluation in a clinical setting to assess their ability to prevent clinically relevant nephrostomy infections.

scholarly journals In VitroActivity of AZD0914, a Novel Bacterial DNA Gyrase/Topoisomerase IV Inhibitor, against Clinically Relevant Gram-Positive and Fastidious Gram-Negative Pathogens

2015 ◽  
Vol 59 (10) ◽  
pp. 6053-6063 ◽  
Author(s):  
Douglas J. Biedenbach ◽  
Michael D. Huband ◽  
Meredith Hackel ◽  
Boudewijn L. M. de Jonge ◽  
Daniel F. Sahm ◽  
...  
Keyword(s):  
Bacterial Species ◽  
Dna Gyrase ◽  
Species Group ◽  
Coagulase Negative Staphylococci ◽  
Topoisomerase Iv ◽  
Gram Positive ◽  
Bacterial Dna ◽  
Gram Negative ◽  
Content Type

ABSTRACTAZD0914, a new spiropyrimidinetrione bacterial DNA gyrase inhibitor with a novel mode of inhibition, has activity against bacterial species commonly cultured from patient infection specimens, including fluoroquinolone-resistant isolates. This study assessed thein vitroactivity of AZD0914 against key Gram-positive and fastidious Gram-negative clinical isolates collected globally in 2013. AZD0914 demonstrated potent activity, with MIC90s for AZD0914 of 0.25 mg/liter againstStaphylococcus aureus(n= 11,680), coagulase-negative staphylococci (n= 1,923), streptococci (n= 4,380), andMoraxella catarrhalis(n= 145), 0.5 mg/liter againstStaphylococcus lugdunensis(n= 120) andHaemophilus influenzae(n= 352), 1 mg/liter againstEnterococcus faecalis(n= 1,241), and 2 mg/liter againstHaemophilus parainfluenzae(n= 70). The activity againstEnterococcus faeciumwas more limited (MIC90, 8 mg/liter). The spectrum and potency of AZD0914 included fluoroquinolone-resistant isolates in each species group, including methicillin-resistant staphylococci, penicillin-resistant streptococci, vancomycin-resistant enterococci, β-lactamase-producingHaemophilusspp., andM. catarrhalis. Based on thesein vitrofindings, AZD0914 warrants further investigation for its utility against a variety of Gram-positive and fastidious Gram-negative bacterial species.

scholarly journals In VitroAntibacterial Activity of AZD0914, a New Spiropyrimidinetrione DNA Gyrase/Topoisomerase Inhibitor with Potent Activity against Gram-Positive, Fastidious Gram-Negative, and Atypical Bacteria

2014 ◽  
Vol 59 (1) ◽  
pp. 467-474 ◽  
Author(s):  
Michael D. Huband ◽  
Patricia A. Bradford ◽  
Linda G. Otterson ◽  
Gregory S. Basarab ◽  
Amy C. Kutschke ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Legionella Pneumophila ◽  
Bacterial Species ◽  
Dna Gyrase ◽  
Cross Resistance ◽  
Gram Positive ◽  
Gram Negative ◽  
Content Type ◽  
Topoisomerase Inhibitor

ABSTRACTAZD0914 is a new spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor with potentin vitroantibacterial activity against key Gram-positive (Staphylococcus aureus,Staphylococcus epidermidis,Streptococcus pneumoniae,Streptococcus pyogenes, andStreptococcus agalactiae), fastidious Gram-negative (Haemophilus influenzaeandNeisseria gonorrhoeae), atypical (Legionella pneumophila), and anaerobic (Clostridium difficile) bacterial species, including isolates with known resistance to fluoroquinolones. AZD0914 works via inhibition of DNA biosynthesis and accumulation of double-strand cleavages; this mechanism of inhibition differs from those of other marketed antibacterial compounds. AZD0914 stabilizes and arrests the cleaved covalent complex of gyrase with double-strand broken DNA under permissive conditions and thus blocks religation of the double-strand cleaved DNA to form fused circular DNA. Whereas this mechanism is similar to that seen with fluoroquinolones, it is mechanistically distinct. AZD0914 exhibited low frequencies of spontaneous resistance inS. aureus, and if mutants were obtained, the mutations mapped togyrB. Additionally, no cross-resistance was observed for AZD0914 against recent bacterial clinical isolates demonstrating resistance to fluoroquinolones or other drug classes, including macrolides, β-lactams, glycopeptides, and oxazolidinones. AZD0914 was bactericidal in both minimum bactericidal concentration andin vitrotime-kill studies. Inin vitrocheckerboard/synergy testing with 17 comparator antibacterials, only additivity/indifference was observed. The potentin vitroantibacterial activity (including activity against fluoroquinolone-resistant isolates), low frequency of resistance, lack of cross-resistance, and bactericidal activity of AZD0914 support its continued development.

scholarly journals Synthesis, antioxidant and antimicrobial activity of carbohydrazones

2017 ◽  
Vol 82 (5) ◽  
pp. 495-508 ◽  
Author(s):  
Aleksandra Bozic ◽  
Nenad Filipovic ◽  
Irena Novakovic ◽  
Snezana Bjelogrlic ◽  
Jasmina Nikolic ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Dimethyl Sulphoxide ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Antioxidant Compound ◽  
Antioxidant And Antimicrobial Activity ◽  
Bacteria And Fungi

Fourteen mono- and bis-carbohydrazone ligands have been synthesized and characterized. Antioxidant activity of the substances was investigated together with possible (E)/(Z) isomerization, and explained on the most active antioxidant compound 4 in various dimethyl sulphoxide?water mixtures. The addition of water to the system was involved in the formation of hydrated molecules which was confirmed in NMR after the addition of D2O. The ligands were tested in vitro against Gram-positive and Gram-negative bacteria and fungi, and their activity was discussed in relation to the structure of investigated carbohydrazone.

scholarly journals Lipid Segregation Explains Selective Toxicity of a Series of Fragments Derived from the Human Cathelicidin LL-37

2009 ◽  
Vol 53 (9) ◽  
pp. 3705-3714 ◽  
Author(s):  
Raquel F. Epand ◽  
Guangshun Wang ◽  
Bob Berno ◽  
Richard M. Epand
Keyword(s):  
Antimicrobial Activity ◽  
Bacterial Species ◽  
Antimicrobial Activities ◽  
Gram Negative Bacteria ◽  
Selective Toxicity ◽  
Gram Positive ◽  
Gram Negative ◽  
Cytoplasmic Membranes ◽  
Anionic Lipids ◽  
Active Segment

ABSTRACT The only human cathelicidin, the 37-residue peptide LL-37, exhibits antimicrobial activity against both gram-positive and gram-negative bacteria. We studied the ability of several fragments of LL-37, exhibiting different antimicrobial activities, to interact with membranes whose compositions mimic the cytoplasmic membranes of gram-positive or of gram-negative bacteria. These fragments are as follows: KR-12, the smallest active segment of LL-37, with the sequence KRIVQRIKDFLR, which exhibits antimicrobial activity only against gram-negative bacteria; a slightly smaller peptide, RI-10, missing the two cationic residues at the N and C termini of KR-12, which has been shown not to have any antimicrobial activity; a longer peptide, GF-17, which shows antimicrobial activity against gram-positive as well as gram-negative bacteria; and GF-17D3, with 3 d-amino-acid residues, which is also selective only for gram-negative bacteria. Those fragments with the capacity to cluster anionic lipids away from zwitterionic lipids in a membrane exhibit selective toxicity toward bacteria containing zwitterionic as well as anionic lipids in their cytoplasmic membranes but not toward bacteria with only anionic lipids. This finding allows for the prediction of the bacterial-species selectivity of certain agents and paves the way for designing new antimicrobials targeted specifically toward gram-negative bacteria.

scholarly journals Synthesis of certain pyrrole derivatives as antimicro-bial agents

2009 ◽  
Vol 59 (2) ◽  
pp. 145-158 ◽  
Author(s):  
Mosaad Mohamed ◽  
Ramdan El-Domany ◽  
Rania Abd El-Hameed
Keyword(s):  
Antimicrobial Activity ◽  
Aromatic Amines ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Pyrrole Derivatives ◽  
Gram Negative ◽  
Primary Aromatic Amines ◽  
Aryl Amines ◽  
Bacteria And Fungi

Synthesis of certain pyrrole derivatives as antimicro-bial agentsIn an effort to establish new pyrroles and pyrrolo[2,3-d] pyrimidines with improved antimicrobial activity we report here the synthesis andin vitromicrobiological evaluation of a series of pyrrole derivatives. A series of new 2-aminopyrrole-3-carbonitriles (1a-d) were synthesized from the reaction of benzoin, primary aromatic amines and malononitrile, from which a number of pyrrole derivatives (2a-dto5a-d) and pyrrolo[2,3-d]pyrimidines (6a-dto10a, d) were synthesized. Thein vitroantimicrobial testing of the synthesized compounds was carried out against Gram-positive, Gram-negative bacteria and fungi. Some of the prepared compounds, [2-amino-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrole-3-carbonitriles (1b), 2-amino-3-carbamoyl-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrroles (2b),N-(3-cyano-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3b),N-(3-cyano-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3c), 2-amino-1-(4-methoxyphenyl)-4,5-diphenyl-3-tetrazolo-1H-pyrroles (5d),7-(4-methoxyphenyl)-5,6-diphenyl-7H-pyrrolo [2,3-d]pyrimidin-4(3H)-ones (7d), 7-(3-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-thione (9b) andN-(7-(2-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d] pyrimidine)-N-aryl amines (10a)] showed potent antimicrobial activity.

scholarly journals Inhibition of Neisseria gonorrhoeae Type II Topoisomerases by the Novel Spiropyrimidinetrione AZD0914

2015 ◽  
Vol 290 (34) ◽  
pp. 20984-20994 ◽  
Author(s):  
Gunther Kern ◽  
Tiffany Palmer ◽  
David E. Ehmann ◽  
Adam B. Shapiro ◽  
Beth Andrews ◽  
...  
Keyword(s):  
Neisseria Gonorrhoeae ◽  
Bacterial Species ◽  
Dna Gyrase ◽  
Resistant Mutant ◽  
Multidrug Resistant ◽  
Type Ii ◽  
Topoisomerase Iv ◽  
Gram Positive ◽  
Gram Negative

We characterized the inhibition of Neisseria gonorrhoeae type II topoisomerases gyrase and topoisomerase IV by AZD0914 (AZD0914 will be henceforth known as ETX0914 (Entasis Therapeutics)), a novel spiropyrimidinetrione antibacterial compound that is currently in clinical trials for treatment of drug-resistant gonorrhea. AZD0914 has potent bactericidal activity against N. gonorrhoeae, including multidrug-resistant strains and key Gram-positive, fastidious Gram-negative, atypical, and anaerobic bacterial species (Huband, M. D., Bradford, P. A., Otterson, L. G., Basrab, G. S., Giacobe, R. A., Patey, S. A., Kutschke, A. C., Johnstone, M. R., Potter, M. E., Miller, P. F., and Mueller, J. P. (2014) In Vitro Antibacterial Activity of AZD0914: A New Spiropyrimidinetrione DNA Gyrase/Topoisomerase Inhibitor with Potent Activity against Gram-positive, Fastidious Gram-negative, and Atypical Bacteria. Antimicrob. Agents Chemother. 59, 467–474). AZD0914 inhibited DNA biosynthesis preferentially to other macromolecules in Escherichia coli and induced the SOS response to DNA damage in E. coli. AZD0914 stabilized the enzyme-DNA cleaved complex for N. gonorrhoeae gyrase and topoisomerase IV. The potency of AZD0914 for inhibition of supercoiling and the stabilization of cleaved complex by N. gonorrhoeae gyrase increased in a fluoroquinolone-resistant mutant enzyme. When a mutation, conferring mild resistance to AZD0914, was present in the fluoroquinolone-resistant mutant, the potency of ciprofloxacin for inhibition of supercoiling and stabilization of cleaved complex was increased greater than 20-fold. In contrast to ciprofloxacin, religation of the cleaved DNA did not occur in the presence of AZD0914 upon removal of magnesium from the DNA-gyrase-inhibitor complex. AZD0914 had relatively low potency for inhibition of human type II topoisomerases α and β.

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