Displaying publications 81 - 100 of 849 in total

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  1. Synthesis of some new N-(alkyl/aralkyl)-N-(4-methoxyphenethyl) benzene sulfonamides as antibacterial agents against Escherichia
    Abbasi MA, Fatima Z, Rehman AU, Siddiqui SZ, Ali Shah SA, Shahid M, et al.
    Pak J Pharm Sci, 2019 Sep;32(5):1957-1964.
    PMID: 31813858
    The present study comprises the synthesis of a new series of benzenesulfonamides derived from N-sulfonation of 2-(4-methoxyphenyl)-1-ethanamine (1). The synthesis was initiated by the reaction of 2-(4-methoxyphenyl)-1-ethanamine (1) with benzenesulfonyl chloride (2), to yield N-(4-methoxyphenethyl)benzenesulfonamide (3). This parent molecule 3 was subsequently treated with various alkyl/aralkyl halides (4a-j) in N,N-dimethylformamide (DMF) and in the presence of a weak base lithium hydride (LiH) to obtain various N-(alkyl/aralkyl)-N-(4-methoxyphenethyl) benzenesulfonamides (5a-j). The characterization of these derivatives was carried out by spectroscopic techniques like IR, 1H-NMR, and 13C-NMR. Elemental analysis also supported this data. The biofilm inhibitory action of all the synthesized compounds was carried out on Escherichia coli and some of the compounds were identified to be very suitable inhibitors of this bacterial strain. Furthermore, the molecules were also tested for their cytotoxicity behavior to assess their utility as less cytotoxic therapeutic agents.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  2. Fulltext Synthesis of silver nanoparticles with antibacterial activity using the lichen Parmotrema praesorediosum
    Mie R, Samsudin MW, Din LB, Ahmad A, Ibrahim N, Adnan SN
    Int J Nanomedicine, 2014;9:121-7.
    PMID: 24379670 DOI: 10.2147/IJN.S52306
    Development of a green chemistry process for the synthesis of silver nanoparticles has become a focus of interest. This would offer numerous benefits, including ecofriendliness and compatibility for biomedical applications. Here we report the synthesis of silver nanoparticles from the reduction of silver nitrate and an aqueous extract of the lichen Parmotrema praesorediosum as a reductant as well as a stabilizer. The physical appearance of these silver nanoparticles was characterized using ultraviolet-visible spectroscopy, electron microscopy, energy-dispersive spectroscopy, and X-ray diffraction techniques. The results show that silver nanoparticles synthesized using P. praesorediosum have an average particle size of 19 nm with a cubic structure. The antibacterial activity of the synthesized silver nanoparticles was tested against eight micro-organisms using the disk diffusion method. The results reveal that silver nanoparticles synthesized using P. praesorediosum have potential antibacterial activity against Gram-negative bacteria.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology
  3. Fulltext Synthesis of silver nanoparticles in montmorillonite and their antibacterial behavior
    Shameli K, Ahmad MB, Zargar M, Yunus WM, Rustaiyan A, Ibrahim NA
    Int J Nanomedicine, 2011;6:581-90.
    PMID: 21674015 DOI: 10.2147/IJN.S17112
    Silver nanoparticles (Ag NPs) were synthesized by the chemical reducing method in the external and interlamellar space of montmorillonite (MMT) as a solid support at room temperature. AgNO(3) and NaBH(4) were used as a silver precursor and reducing agent, respectively. The most favorable experimental conditions for synthesizing Ag NPs in the MMT are described in terms of the initial concentration of AgNO(3). The interlamellar space limits changed little (d-spacing = 1.24-1.47 nm); therefore, Ag NPs formed on the MMT suspension with d-average = 4.19-8.53 nm diameter. The Ag/MMT nanocomposites (NCs), formed from AgNO(3)/MMT suspension, were characterizations with different instruments, for example UV-visible, PXRD, TEM, SEM, EDXRF, FT-IR, and ICP-OES analyzer. The antibacterial activity of different sizes of Ag NPs in MMT were investigated against Gram-positive, ie, Staphylococcus aureus and methicillin-resistant S. aureus (MRSA) and Gram-negative bacteria, ie, Escherichia coli, Escherichia coli O157:H7, and Klebsiella pneumoniae, by the disk diffusion method using Mueller-Hinton agar (MHA). The smaller Ag NPs were found to have significantly higher antibacterial activity. These results showed that Ag NPs can be used as effective growth inhibitors in different biological systems, making them applicable to medical applications.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  4. Synthesis of halogenated azo-aspirin analogues from natural product derivatives as the potential antibacterial agents
    Ngaini Z, Mortadza NA
    Nat Prod Res, 2019 Dec;33(24):3507-3514.
    PMID: 29911437 DOI: 10.1080/14786419.2018.1486310
    Chemical modification of medicines from natural product-based molecules has become of interest in recent years. In this study, a series of halogenated azo derivatives 1a-d were synthesised via coupling reaction, followed by Steglich esterification with aspirin (a natural product derivative) to form azo derivatives 2a-d. While, halogenated azo-aspirin 3a-d were synthesised via direct coupling reaction of aspirin and diazonium salt. Bacteriostatic activity was demonstrated against E. coli and S. aureus via turbidimetric kinetic method. Compound 3a-d showed excellent antibacterial activities against E. coli (MIC 75-94 ppm) and S. aureus (MIC 64-89 ppm) compared to ampicillin (MIC 93 and 124 ppm respectively), followed by 1a-d and 2a-d. The presence of reactive groups of -OH, N=N, C=O and halogens significantly contribute excellent interaction towards E. coli and S. aureus. Molecular dockings analysis of 3a against MIaC protein showed binding free energy of -7.2 kcal/mol (E. coli) and -6.6 kcal/mol (S. aureus).
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  5. Synthesis of Pectin and Eggshell Biowaste-Mediated Nano-hydroxyapatite (nHAp), Their Physicochemical Characterizations, and Use as Antibacterial Material
    Thakur P, Arivarasan VK, Kumar G, Pant G, Kumar R, Pandit S, et al.
    Appl Biochem Biotechnol, 2024 Jan;196(1):491-505.
    PMID: 37145344 DOI: 10.1007/s12010-023-04550-6
    The current study reports the synthesis of sustainable nano-hydroxyapatite (nHAp) using a wet chemical precipitation approach. The materials used in the green synthesis of nHAp were obtained from environmental biowastes such as HAp from eggshells and pectin from banana peels. The physicochemical characterization of obtained nHAp was carried out using different techniques. For instance, X-ray diffractometer (XRD) and FTIR spectroscopy were used to study the crystallinity and synthesis of nHAp respectively. In addition, the morphology and elemental composition of nHAP were studied using FESEM equipped with EDX. HRTEM showed the internal structure of nHAP and calculated its grain size which was 64 nm. Furthermore, the prepared nHAp was explored for its antibacterial and antibiofilm activity which has received less attention previously. The obtained results showed the potential of pectin-bound nHAp as an antibacterial agent for various biomedical and healthcare applications.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology
  6. Synthesis of Iron Oxide@Pt Core-Shell Nanoparticles for Reductive Conversion of Cr(VI) to Cr(III) and Antibacterial Studies
    Sivaranjan K, Santhanalakshmi J, Panneer DS, Vivekananthan S, Sagadevan S, Johan MRB, et al.
    J Nanosci Nanotechnol, 2020 02 01;20(2):918-923.
    PMID: 31383087 DOI: 10.1166/jnn.2020.16895
    Herein, we report the facile synthesis of Iron oxide@Pt core-shell nanoparticles (NPs) by facile two step synthesis process. The first step follows the growth of iron oxide nanoparticle by thermal decomposition process while the second step deals with the formation of iron oxide@Pt core-shell nanoparticles by the chemical reduction method. The synthesized core-shell nanoparticles were characterized by several techniques and used for the catalytic reductive translation of Cr(VI) to Cr(III) in the presence of formic acid by a UV-vis spectrophotometer. The UV photo-spectrometer analysis confirmed the conversion efficiency from 12% to as high as 98.8% at the end of 30 minutes. Thus, the presence of Iron oxide @Pt core-shell nanoparticles (NPs) can be effectively used as a catalyst for the reducion of Cr(VI) to Cr(III) ions. Additionally, antibacterial studies were performed for the prepared core-shell nanoparticles against two bacterial strains, i.e., gram (+ve) Staphylococcus Aureus (S. Aureus) and gram (-ve) Escherichia Coli (E. Coli).
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology
  7. Fulltext Synthesis of 4-(dimethylamino)pyridine propylthioacetate coated gold nanoparticles and their antibacterial and photophysical activity
    Anwar A, Khalid S, Perveen S, Ahmed S, Siddiqui R, Khan NA, et al.
    J Nanobiotechnology, 2018 Jan 29;16(1):6.
    PMID: 29378569 DOI: 10.1186/s12951-017-0332-z
    BACKGROUND: Gold nanoparticles are useful candidate for drug delivery applications and are associated with enhancement in the bioavailability of coated drugs and/or therapeutic agent. Since, heterocyclic compounds are known to exhibit antimicrobial potential against variety of pathogens, we designed this study to evaluate the antibacterial effects of gold nanoparticles conjugation with new synthesized cationic ligand; 4-Dimethyl aminopyridinium propylthioacetate (DMAP-PTA) in comparison with pure compound and antibiotic drug Pefloxacin. Antibacterial activity of DMAP-PTA coated gold nanoparticles was investigated against a fecal strain of E. coli (ATCC 8739).

    RESULTS: A new dimethyl aminopyridine based stabilizing agent named as DMAP-PTA was synthesized and used for stabilization of gold nanoparticles. Gold nanoparticles coated with DMAP-PTA abbreviated as DMAP-PTA-AuNPs were thoroughly characterized by UV-visible, FT-IR spectroscopic methods and transmission electron microscope before biological assay. DMAP-PTA, DMAP-PTA-AuNPs and Pefloxacin were examined for their antibacterial potential against E. coli, and the minimum inhibitory concentration (MIC) was determined to be 300, 200 and 50 µg/mL respectively. Gold nanoparticles conjugation was found to significantly enhance the antibacterial activity of DMAP-PTA as compared to pure compound. Moreover, effects of DMAP-PTA-AuNPs on the antibacterial potential of Pefloxacin was also evaluated by combination therapy of 1:1 mixture of DMAP-PTA-AuNPs and Pefloxacin against E. coli in a wide range of concentrations from 5 to 300 µg/mL. The MIC of Pefloxacin + DMAP-PTA-AuNPs mixture was found to be 25 µg/mL as compared to Pefloxacin alone (50 µg/mL), which clearly indicates that DMAP-PTA-AuNPs increased the potency of Pefloxacin. AFM analysis was also carried out to show morphological changes occur in bacteria before and after treatment of test samples. Furthermore, DMAP-PTA-AuNPs showed high selectivity towards Pefloxacin in spectrophotometric drug recognition studies which offers tremendous potential for analytical applications.

    CONCLUSIONS: Gold nanoparticles conjugation was shown to enhance the antibacterial efficacy of DMAP-PTA ligand, while DMAP-PTA-AuNPs also induced synergistic effects on the potency of Pefloxacin against E. coli. DMAP-PTA-AuNPs were also developed as Pefloxacin probes in recognizing the drug in blood and water samples in the presence of other drugs.

    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  8. Synthesis of 2-Furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives as suitable antibacterial agents with mild cytotoxicity
    Abbasi MA, Nazeer MM, Rehman A, Siddiqui SZ, Hussain G, Shah SA, et al.
    Pak J Pharm Sci, 2018 Nov;31(6):2477-2485.
    PMID: 30473521
    The aim of the present research work was synthesis of some 2-furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives and to ascertain their antibacterial potential. The cytotoxicity of these molecules was also checked to find out their utility as possible therapeutic agents. The synthesis was initiated by reacting furyl(-1-piperazinyl)methanone (1) in N,N-dimethylformamide (DMF) and lithium hydride with different aralkyl halides (2a-j) to afford 2-furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives (3a-j). The structural confirmation of all the synthesized compounds was done by IR, EI-MS, 1H-NMR and 13C-NMR spectral techniques and through elemental analysis. The results of in vitro antibacterial activity of all the synthesized compounds were screened against Gram-negative (S. typhi, E. coli, P. aeruginosa) and Gram-positive (B. subtilis, S. aureus) bacteria and were found to be decent inhibitors. Amongst the synthesized molecules, 3e showed lowest minimum inhibitory concentration MIC = 7.52±0.μg/mL against S. Typhi, credibly due to the presence of 2-bromobenzyl group, relative to the reference standard, ciprofloxacin, having MIC = 7.45±0.58μg/mL.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  9. Synthesis and in vitro Bioactivity Evaluation of New Galactose and Fructose Ester Derivatives of 5-Aminosalicylic Acid
    Yousefi S, Bayat S, Rahman MB, Ibrahim Z, Abdulmalek E
    Chem Biodivers, 2017 Apr;14(4).
    PMID: 28036129 DOI: 10.1002/cbdv.201600362
    Inflammatory bowel disease (IBD) is the main risk factor for developing colorectal cancer which is common in patients of all ages. 5-Aminosalicylic acid (5-ASA), structurally related to the salicylates, is highly active in the treatment of IBD with minor side effects. In this study, the synthesis of galactose and fructose esters of 5-ASA was planned to evaluate the role of glycoconjugation on the bioactivity of the parent drug. The antibacterial activity of the new compounds were evaluated against two Gram-negative and two Gram-positive species of bacteria, with a notable effect observed against Staphylococcus aureus and Escherichia coli in comparisons with the 5-ASA. Cytotoxicity testing over HT-29 and 3T3 cell lines indicated that the toxicity of the new products against normal cells was significantly reduced compared with the original drug, whereas their activity against cancerous cells was slightly decreased. The anti-inflammatory activity test in RAW264.7 macrophage cells indicated that the inhibition of nitric oxide by both of the monosaccharide conjugated derivatives was slightly improved in comparison with the non-conjugated drug.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology
  10. Synthesis and evaluation of antibacterial activity of transition metal-oleoyl amide complexes
    Farhan N, Al-Maleki AR, Sarih NM, Yahya R
    Bioorg Chem, 2023 Nov;140:106786.
    PMID: 37586131 DOI: 10.1016/j.bioorg.2023.106786
    Recent studies show that some metal ions, injure microbial cells in various ways due to membrane breakdown, protein malfunction, and oxidative stress. Metal complexes are suited for creating novel antibacterial medications due to their distinct mechanisms of action and the variety of three-dimensional geometries they can acquire. In this Perspective, the present study focused on new antibacterial strategies based on metal oleoyl amide complexes. Thus, oleoyl amides ligand (fatty hydroxamic acid and fatty hydrazide hydrate) with the transition metal ions named Ag (I), Co (II), Cu (II), Ni (II) and Sn (II) complexes were successfully synthesized in this study. The metals- oleoyl amide were characterized using elemental analysis, and fourier transforms infrared (FTIR) spectroscopy. The antibacterial effect of metals- oleoyl amide complexes was investigated for Gram-negative bacteria (Escherichia coli) and Gram-positive bacteria (Staphylococcus aureus) by analysing minimum inhibitory concentration (MIC), minimal bactericidal concentration (MBC), and scanning electron microscopy (SEM). The results showed that metal-oleoyl amide complexes have high antibacterial activity at low concentrations. This study inferred that metal oleoyl amide complexes could be utilised as a promising therapeutic antibacterial agent.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology
  11. Fulltext Synthesis and characterization of silver/montmorillonite/chitosan bionanocomposites by chemical reduction method and their antibacterial activity
    Shameli K, Bin Ahmad M, Zargar M, Yunus WM, Ibrahim NA, Shabanzadeh P, et al.
    Int J Nanomedicine, 2011;6:271-84.
    PMID: 21499424 DOI: 10.2147/IJN.S16043
    Silver nanoparticles (AgNPs) of a small size were successfully synthesized using the wet chemical reduction method into the lamellar space layer of montmorillonite/chitosan (MMT/Cts) as an organomodified mineral solid support in the absence of any heat treatment. AgNO3, MMT, Cts, and NaBH4 were used as the silver precursor, the solid support, the natural polymeric stabilizer, and the chemical reduction agent, respectively. MMT was suspended in aqueous AgNO3/Cts solution. The interlamellar space limits were changed (d-spacing = 1.24-1.54 nm); therefore, AgNPs formed on the interlayer and external surface of MMT/Cts with d-average = 6.28-9.84 nm diameter. Characterizations were done using different methods, ie, ultraviolet-visible spectroscopy, powder X-ray diffraction, transmission electron microscopy, scanning electron microscopy, energy dispersive X-ray fluorescence spectrometry, and Fourier transform infrared spectroscopy. Silver/montmorillonite/chitosan bionanocomposite (Ag/MMT/Cts BNC) systems were examined. The antibacterial activity of AgNPs in MMT/Cts was investigated against Gram-positive bacteria, ie, Staphylococcus aureus and methicillin-resistant S. aureus and Gram-negative bacteria, ie, Escherichia coli, E. coli O157:H7, and Pseudomonas aeruginosa by the disc diffusion method using Mueller Hinton agar at different sizes of AgNPs. All of the synthesized Ag/MMT/Cts BNCs were found to have high antibacterial activity. These results show that Ag/MMT/Cts BNCs can be useful in different biological research and biomedical applications, including surgical devices and drug delivery vehicles.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  12. Synthesis and characterization of nitrile functionalized silver(I)-N-heterocyclic carbene complexes: DNA binding, cleavage studies, antibacterial properties and mosquitocidal activity against the dengue vector, Aedes albopictus
    Asekunowo PO, Haque RA, Razali MR, Avicor SW, Wajidi MFF
    Eur J Med Chem, 2018 Apr 25;150:601-615.
    PMID: 29550733 DOI: 10.1016/j.ejmech.2018.03.029
    A series of four benzimidazolium based nitrile-functionalized mononuclear-Ag(I)-N-heterocyclic carbene and binuclear-Ag(I)-N-heterocyclic carbene (Ag(I)-NHC) hexafluorophosphate complexes (5b-8b) were synthesized by reacting the corresponding hexafluorophosphate salts (1b-4b) with Ag2O in acetonitrile, respectively. These compounds were characterized by 1H NMR, 13C NMR, IR, UV-visible spectroscopic techniques, elemental analyses and molar conductivity. Additionally, 8b was structurally characterized by single crystal X-ray diffraction technique. Preliminary in vitro antibacterial evaluation was conducted for all the compounds against two standard bacteria; gram-positive (Staphylococcus aureus) and gram-negative (Escherichia coli) bacterial strains. Most of the Ag(I)-NHC complexes (5b-8b) showed moderate to good antibacterial activity with MIC values in the range of 12.5-100 μg/mL. Especially, compound 8b exhibited promising anti-Staphylococcus aureus activity with a low MIC value (12.5 μg/mL). However, all the hexafluorophosphate salts (1b-4b) were inactive against the bacteria strains. The preliminary interactive investigation revealed that the most active compound, 8b, could effectively intercalate into DNA to form 8b-DNA complex which shows a better binding ability for DNA (Kb = 3.627 × 106) than the complexes 5b-7b (2.177 × 106, 8.672 × 105 and 6.665 × 105, respectively). Nuclease activity of the complexes on plasmid DNA and Aedes albopictus genomic DNA was time-dependent, although minimal. The complexes were larvicidal to the mosquito, with 5b, 6b and 8b being highly active. Developmental progression from the larval to the adult stage was affected by the complexes, progressively being toxic to the insect's development with increasing concentration. These indicate the potential use of these complexes as control agents against bacteria and the dengue mosquito Ae. albopictus.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  13. Synthesis and characterization of marine seagrass (Cymodocea serrulata) mediated titanium dioxide nanoparticles for antibacterial, antibiofilm and antioxidant properties
    Narayanan M, Srinivasan S, Gnanasekaran C, Ramachandran G, Chelliah CK, Rajivgandhi G, et al.
    Microb Pathog, 2024 Apr;189:106595.
    PMID: 38387848 DOI: 10.1016/j.micpath.2024.106595
    Cymodocea serrulata mediated titanium dioxide nanoparticles (TiO2 NPs) were successfully synthesized. The XRD pattern and FTIR spectra demonstrated the crystalline structure of TiO2 NPs and the presence of phenols, flavonoids and alkaloids in the extract. Further SEM revealed that TiO2 NPs has uniform structure and spherical in shape with their size ranged from 58 to 117 nm. Antibacterial activity of TiO2 NPs against methicillin-resistant Staphylococcus aureus (MRSA) and Vibrio cholerae (V. cholerae), provided the zone of inhibition of 33.9 ± 1.7 and 36.3 ± 1.9 mm, respectively at 100 μg/mL concentration. MIC of TiO2 NPs against MRSA and V. cholerae showed 84% and 87% inhibition at 180 μg/mL and 160 μg/mL respectively. Subsequently, the sub-MIC of V. cholerae demonstrated minimal or no impact on bacterial growth at concentration of 42.5 μg/mL concentration. In addition, TiO2 NPs exhibited their ability to inhibit the biofilm forming V. cholerae which caused distinct morphological and intercellular damages analysed using CLSM and TEM. The antioxidant properties of TiO2 NPs were demonstrated through TAA and DPPH assays and exposed its scavenging activity with IC50 value of 36.42 and 68.85 μg/mL which denotes its valuable antioxidant properties with potential health benefits. Importantly, the brine shrimp based lethality experiment yielded a low cytotoxic effect with 13% mortality at 100 μg/mL. In conclusion, the multifaceted attributes of C. serrulata mediated TiO2 NPs encompassed the antibacterial, antioxidant and anti-biofilm inhibition effects with low cytotoxicity in nature were highlighted in this study and proved the bioderived TiO2 NPs could be used as a promising agent for biomedical applications.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology
  14. Synthesis and characterization of 4-nitro benzaldehyde with ZnO-based nanoparticles for biomedical applications
    Indumathi T, Kumaresan I, Suriyaprakash J, Alarfaj AA, Hirad AH, Jaganathan R, et al.
    J Basic Microbiol, 2024 Feb;64(2):e2300494.
    PMID: 37988661 DOI: 10.1002/jobm.202300494
    Globally, cancer is the leading cause of death and morbidity, and skin cancer is the most common cancer diagnosis. Skin problems can be treated with nanoparticles (NPs), particularly with zinc oxide (ZnO) NPs, which have antioxidant, antibacterial, anti-inflammatory, and anticancer properties. An antibacterial activity of zinc oxide nanoparticles prepared in the presence of 4-nitrobenzaldehyde (4NB) was also tested in the present study. In addition, the influence of synthesized NPs on cell apoptosis, cell viability, mitochondrial membrane potential (MMP), endogenous reactive oxygen species (ROS) production, apoptosis, and cell adhesion was also examined. The synthesized 4-nitro benzaldehyde with ZnO (4NBZnO) NPs were confirmed via characterization techniques. 4NBZnO NPs showed superior antibacterial properties against the pathogens tested in antibacterial investigations. As a result of dose-based treatment with 4NBZnO NPs, cell viability, and MMP activity of melanoma cells (SK-MEL-3) cells were suppressed. A dose-dependent accumulation of ROS was observed in cells exposed to 4NBZnO NPs. As a result of exposure to 4NBZnO NPs in a dose-dependent manner, viable cells declined and apoptotic cells increased. This indicates that apoptotic cell death was higher. The cell adhesion test revealed that 4NBZnO NPs reduced cell adhesion and may promote apoptosis of cancer cells because of enhanced ROS levels.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology
  15. Synthesis and biological evaluation of novel substituted 1,3,4-thiadiazole and 2,6-di aryl substituted imidazo [2,1-b] [1,3,4] thiadiazole derivatives
    Chandrakantha B, Isloor AM, Shetty P, Fun HK, Hegde G
    Eur J Med Chem, 2014 Jan;71:316-23.
    PMID: 24321835 DOI: 10.1016/j.ejmech.2013.10.056
    A new series of N-[5-(4-(alkyl/aryl)-3-nitro-phenyl)-[1,3,4-thiadiazol-2-yl]-2,2-dimethyl-propionamide 4 (a-l) and 6-(4-Methoxy-phenyl)-2-(4-alkyl/aryl)-3-nitro-phenyl)-Imidazo [2,1-b] [1,3,4] thiadiazole 6 (a-l) were synthesized starting from 5-(4-Fluoro-3-nitro-phenyl)-[1,3,4] thiadiazole-2-ylamine. The synthesized compounds were characterized by IR, NMR, mass spectral and elemental analysis. All the compounds were tested for antibacterial and antifungal activities. The antimicrobial activities of the compounds were assessed by well plate method (zone of inhibition). Compounds 4a, 4c and 6e, 6g displayed appreciable activity at the concentration 0.5-1.0 mg/mL.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  16. Synthesis and biological evaluation of indole core-based derivatives with potent antibacterial activity against resistant bacterial pathogens
    Hong W, Li J, Chang Z, Tan X, Yang H, Ouyang Y, et al.
    J Antibiot (Tokyo), 2017 Jul;70(7):832-844.
    PMID: 28465626 DOI: 10.1038/ja.2017.55
    The emergence of drug resistance in bacterial pathogens is a growing clinical problem that poses difficult challenges in patient management. To exacerbate this problem, there is currently a serious lack of antibacterial agents that are designed to target extremely drug-resistant bacterial strains. Here we describe the design, synthesis and antibacterial testing of a series of 40 novel indole core derivatives, which are predicated by molecular modeling to be potential glycosyltransferase inhibitors. Twenty of these derivatives were found to show in vitro inhibition of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus. Four of these strains showed additional activity against Gram-negative bacteria, including extended-spectrum beta-lactamase producing Enterobacteriaceae, imipenem-resistant Klebsiella pneumoniae and multidrug-resistant Acinetobacter baumanii, and against Mycobacterium tuberculosis H37Ra. These four compounds are candidates for developing into broad-spectrum anti-infective agents.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  17. Synthesis and antimicrobial studies of hydroxylated chalcone derivatives with variable chain length
    Ngaini Z, Fadzillah SM, Hussain H
    Nat Prod Res, 2012;26(10):892-902.
    PMID: 21678160 DOI: 10.1080/14786419.2010.502896
    A series of (E)-1-(4-alkyloxyphenyl)-3-(hydroxyphenyl)-prop-2-en-1-one have been successfully synthesised via Claisen-Schmidt condensation. The synthesised chalcone derivatives consisted of hydroxyl groups at either ortho, meta or para position and differed in the length of the alkyl groups, C (n) H(2) (n) (+1,) where n = 6, 10, 12 and 14. The structures of all compounds were defined by elemental analysis, IR, (1)H- and (13)C-NMR. The antimicrobial studies were carried out against wild-type Escherichia coli American Type Culture Collection 8739 to evaluate the effect of the hydroxyl and the alkyl groups of the synthesised chalcones. All the synthesised compounds have shown significant antimicrobial activities. The optimum inhibition was dependent on the position of the hydroxyl group as well as the length of the alkyl chains.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  18. Synthesis and anti-microbial potencies of 1-(2-hydroxyethyl)-3-alkylimidazolium chloride ionic liquids: microbial viabilities at different ionic liquids concentrations
    Hossain MI, El-Harbawi M, Alitheen NB, Noaman YA, Lévêque JM, Yin CY
    Ecotoxicol Environ Saf, 2013 Jan;87:65-9.
    PMID: 23107478 DOI: 10.1016/j.ecoenv.2012.09.020
    Three 1-(2-hydroxyethyl)-3-alkylimidazolium chloride room temperature ionic liquids (ILs) [2OHimC(n)][Cl]; (n=0, 1, 4) have been synthesized from the appropriate imidazole precursors and characterized by IR and NMR spectroscopies and elemental analysis. Their anti-microbial activities were investigated using the well-diffusion method. The viabilities of Escherichia coli, Aeromonas hydrophila, Listeria monocytogenes and Salmonella enterica as a function of IL concentrations were studied. The minimal inhibitory concentrations (MICs) and EC₅₀ values for the present ILs were within the concentration range from 60 to 125 mM and 23 to 73 mM. The anti-microbial potencies of the present ILs were compared to a standard antibiotic, gentamicin. The finding affords additional perspective on the level of ILs toxicity to aquatic lifeforms and yet, this characteristic can be readily harnessed to detect microbial growth and activity.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
  19. Synthesis and Staphylococcus aureus biofilm inhibitory activity of indolenine-substituted pyrazole and pyrimido[1,2-b]indazole derivatives
    Yap CH, Ramle AQ, Lim SK, Rames A, Tay ST, Chin SP, et al.
    Bioorg Med Chem, 2023 Nov 15;95:117485.
    PMID: 37812886 DOI: 10.1016/j.bmc.2023.117485
    Staphylococcus aureus is a highly adaptable opportunistic pathogen that can form biofilms and generate persister cells, leading to life-threatening infections that are difficult to treat with antibiotics alone. Therefore, there is a need for an effective S. aureus biofilm inhibitor to combat this public health threat. In this study, a small library of indolenine-substituted pyrazoles and pyrimido[1,2-b]indazole derivatives were synthesised, of which the hit compound exhibited promising antibiofilm activities against methicillin-susceptible S. aureus (MSSA ATCC 29213) and methicillin-resistant S. aureus (MRSA ATCC 33591) at concentrations significantly lower than the planktonic growth inhibition. The hit compound could prevent biofilm formation and eradicate mature biofilms of MSSA and MRSA, with a minimum biofilm inhibitory concentration (MBIC50) value as low as 1.56 µg/mL and a minimum biofilm eradication concentration (MBEC50) value as low as 6.25 µg/mL. The minimum inhibitory concentration (MIC) values of the hit compound against MSSA and MRSA were 50 µg/mL and 25 µg/mL, respectively, while the minimum bactericidal concentration (MBC) values against MSSA and MRSA were > 100 µg/mL. Preliminary structure-activity relationship analysis reveals that the fused benzene ring and COOH group of the hit compound are crucial for the antibiofilm activity. Additionally, the compound was not cytotoxic to human alveolar A549 cells, thus highlighting its potential as a suitable candidate for further development as a S. aureus biofilm inhibitor.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology
  20. Synergy of flavone with vancomycin and oxacillin against vancomycin-intermediate Staphyloccus aureus
    Bakar NS, Zin NM, Basri DF
    Pak J Pharm Sci, 2012 Jul;25(3):633-8.
    PMID: 22713953
    This study evaluated in vitro activity of 9 flavonoids in combination with vancomycin or oxacillin against vancomycin-intermediate Staphylococcus aureus (VISA) ATCC 700699 by employing the checkerboard method to obtain Minimal inhibitory concentration (MIC) and fractional inhibitory concentration (FIC) index. Six flavonoids namely hesperitin, rutin, naringenin, flavones, naringin and 3, 7-dihyroxyflavone which exhibited notable inhibitory activity (MIC values < 3200 μg/ml) were further evaluated for combination assay with antibiotics. The combinations of vancomycin+flavone and oxacillin+flavone were found synergistic with the FIC index value 0.094 and 0.126, respectively. Other combinations showed an additive interaction (FIC index = 1.063) but no antagonistic reaction (FIC index > 4) were observed. In time kill studies, oxacillin-flavone combination at synergistic concentration demonstrated bactericidal effect at 24 h period with concentration-dependent manner on the VISA strain. Following 1 h exposure, the combination also produced persistent effect on the bacteria growth for 2.9 hrs at 1x sub-MIC and more than 24 h at 5x of sub-MIC and there was a significant difference between both concentrations (p<0.05). Vancomycin-flavone combination, however, showed no concentration-dependent effect and lower PAE values (1.159 h and 2.322 h at 1x and 5x sub-MIC, respectively) on the VISA strain. In conclusion, flavone markedly intensifies the susceptibility of oxacillin against VISA and the combination can be implicated for further interaction studies at molecular level.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*
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