Displaying publications 1 - 20 of 56 in total

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  1. 2-Mercaptobenzimidazole Schiff Bases: Design, Synthesis, Antimicrobial Studies and Anticancer Activity on HCT-116 Cell Line
    Tahlan S, Narasimhan B, Lim SM, Ramasamy K, Mani V, Shah SAA
    Mini Rev Med Chem, 2019;19(13):1080-1092.
    PMID: 30306865 DOI: 10.2174/1389557518666181009151008
    BACKGROUND: Increased rate of mortality due to the development of resistance to currently available antimicrobial and anticancer agents initiated the need to develop new chemical entities for the treatment of microbial infections and cancer.

    OBJECTIVE: The present study was aimed to synthesize and evaluate antimicrobial and anticancer activities of Schiff bases of 2-mercaptobenzimidazole.

    METHODS: The Schiff bases of 2-mercaptobenzimidazole were synthesized from 4-(2-(1H-benzo[d]- imidazol-2-ylthio)acetamido)benzohydrazide. The synthesized compounds were evaluated for antimicrobial and anticancer activities by tube dilution method and Sulforhodamine-B (SRB) assay, respectively.

    RESULTS: Compounds 8 (MICpa, an = 2.41, 1.20 µM/ml), 10 (MICse, sa = 2.50 µM/ml), 20 (MICec = 2.34 µM/ml) and 25 (MICca = 1.46 µM/ml) showed significant antimicrobial activity against tested bacterial and fungal strains and compounds 20 (IC50 = 8 µg/ml) and 23 (IC50 = 7 µg/ml) exhibited significant anticancer activity.

    CONCLUSION: In general, the synthesized derivatives exhibited moderate antimicrobial and anticancer activities. Compounds 8 and 25 having high antifungal potential among the synthesized compounds may be taken as lead molecules for the development of novel antifungal agents.

    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  2. A facile stereoselective synthesis of dispiro-indeno pyrrolidine/pyrrolothiazole-thiochroman hybrids and evaluation of their antimycobacterial, anticancer and AchE inhibitory activities
    Bharkavi C, Vivek Kumar S, Ashraf Ali M, Osman H, Muthusubramanian S, Perumal S
    Bioorg Med Chem, 2016 11 15;24(22):5873-5883.
    PMID: 27687968 DOI: 10.1016/j.bmc.2016.09.044
    A facile stereoselective synthesis of novel dispiro indeno pyrrolidine/pyrrolothiazole-thiochroman hybrids has been achieved by 1,3-dipolar cycloaddition of azomethine ylides, generated in situ from ninhydrin and sarcosine/thiaproline, on a series of 3-benzylidenethiochroman-4-ones. The synthesised compounds were screened for their antimycobacterial, anticancer and AchE inhibition activities. Compound 4l (IC50 1.07μM) has been found to exhibit the most potent antimycobacterial activity compared to cycloserine (12 times), pyrimethamine (37 times) and ethambutol (IC50 <1.56μM) and 6l (IC50=2.87μM) is more active than both cycloserine (4 times) and pyrimethamine (12 times). Three compounds, 4a, 6b and 6i, display good anticancer activity against CCRF-CEM cell lines. Compounds 6g and 4g display maximum AchE inhibitory activity with IC50 values of 1.10 and 1.16μmol/L respectively.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  3. A facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines acting as antimycobacterial agents
    Wei AC, Ali MA, Yoon YK, Ismail R, Choon TS, Kumar RS
    Bioorg Med Chem Lett, 2013 Mar 1;23(5):1383-6.
    PMID: 23352268 DOI: 10.1016/j.bmcl.2012.12.069
    A series of fourteen dispiropyrrolidines were synthesized using [3+2]-cycloaddition reactions and were screened for their antimycobacterial activity against Mycobacterium tuberculosis H(37)Rv in HTS (High Throughput Screen). Most of the compounds showed moderate to good activity with MIC of less than 20 μM. Compound 4'-(4-bromophenyl)-1'-methyldispiro[acenaphthylene-1,2'-pyrrolidine-3',2″-indane]-2,1″(1H)-dione (4c) was found to be the most active with MIC of 12.50 μM.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis*
  4. A facile ultrasonic-aided biosynthesis of ZnO nanoparticles using Vaccinium arctostaphylos L. leaf extract and its antidiabetic, antibacterial, and oxidative activity evaluation
    Bayrami A, Alioghli S, Rahim Pouran S, Habibi-Yangjeh A, Khataee A, Ramesh S
    Ultrason Sonochem, 2019 Jul;55:57-66.
    PMID: 31084791 DOI: 10.1016/j.ultsonch.2019.03.010
    The synthesis of nanoparticles often result in the generation of harmful chemical pollutants. As such, many researchers have focused on developing green processes, which include the biosynthesis. In this research, ZnO nanoparticles were prepared using the leaf extract of whortleberry (Vaccinium arctostaphylos L.) via a simple ultrasonic-assisted method. The morphology, crystal size and structure, surface, thermal, and optical properties of the bio-mediated ZnO sample (ZnOext) were analyzed and compared with that produced without incorporating the extract (ZnOchem). The ZnO samples were evaluated for their antidiabetic, antibacterial, as well as their sono- and photo-catalytic performances. Initially, the samples were intraperitoneal injected to alloxan-diabetic rats to examine their treatment efficiency in terms of effects on fasting blood glucose, insulin, cholesterol, high-density lipoprotein, and total triglyceride levels. The ZnOext showed significantly higher efficiency for improving the health status of alloxan-diabetic rats in contrast with other tested treatments, vis. ZnOchem, insulin, and only leaf extract. In addition, both the ZnO samples were assessed against gram-negative and gram-positive bacteria and through sono- and photo-catalytic processes for removing rhodamine B, respectively. The results of this study indicated that not only the ZnOext sample was pollution free, it also exhibited higher potentials for treating diabetic rats, bacterial decontamination, and also oxidative removal of organic compounds under the influences of ultrasound and UV irradiations when compared with ZnOchem sample.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  5. Acridine-based (thio)semicarbazones and hydrazones: Synthesis, in vitro urease inhibition, molecular docking and in-silico ADME evaluation
    Isaac IO, Al-Rashida M, Rahman SU, Alharthy RD, Asari A, Hameed A, et al.
    Bioorg Chem, 2019 02;82:6-16.
    PMID: 30267972 DOI: 10.1016/j.bioorg.2018.09.032
    Urease is a bacterial enzyme that is responsible for virulence of various pathogenic bacteria such as Staphylococcus aureus, Proteus mirabilis, Klebsiella pneumoniae, Ureaplasma urealyticum, Helicobacter pylori and Mycobacterium tuberculosis. Increased urease activity aids in survival and colonization of pathogenic bacteria causing several disorders especially gastric ulceration. Hence, urease inhibitors are used for treatment of such diseases. In search of new molecules with better urease inhibitory activity, herein we report a series of acridine derived (thio)semicarbazones (4a-4e, 6a-6l) that were found to be active against urease enzyme. Molecular docking studies were carried out to better comprehend the preferential mode of binding of these compounds against urease enzyme. Docking against urease from pathogenic bacterium S. pasteurii was also carried out with favorable results. In silico ADME evaluation was done to determine drug likeness of synthesized compounds.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  6. Ameliorative effect of Albizia chinensis synthesized ZnO-NPs on Mycoplasma pneumoniae infected pneumonia mice model
    Yu L, Lu M, Zhang W, Alarfaj AA, Hirad AH, Zhang H
    Microb Pathog, 2020 Apr;141:103960.
    PMID: 31953224 DOI: 10.1016/j.micpath.2019.103960
    BACKGROUND: Mycoplasma pneumoniae (MP) is a common cause of community-acquired pneumonia (CAP) among the children and adults that results upper and lower respiratory tract infections.

    OBJECTIVE: This study was aimed to inspect the ameliorative action of A. chinensis synthesized ZnONPs against M. pneumoniae infected pneumonia mice model.

    MATERIALS AND METHODS: ZnO NPs was synthesized from Albizia chinensis bark extract and characterized by UV-Vis spectroscopy, Fourier Transform Infrared (FTIR), Transmission Electron Microscopy (TEM), energy dispersive X-ray (EDX) and atomic force microscope (AFM) analyses. The antibacterial effectual of synthesized ZnONPs were examined against clinical pathogens. The pneumonia was induced to BALB/c mice via injecting the M. pneumoniae and treated with synthesized ZnONPs, followed by the total protein content, total cell counts and inflammatory mediators level was assessed in the BALF of experimental animals. The Histopathological investigation was done in the lung tissues of test animals.

    RESULTS: The outcomes of this work revealed that the formulated ZnONPs was quasi-spherical, radial and cylindrical; the size was identified as 116.5 ± 27.45 nm in diameter. The in vitro antimicrobial potential of formulated ZnO-NPs displayed noticeable inhibitory capacity against the tested fungal and bacterial strains. The administration of synthesized ZnO-NPs in MP infected mice model has significantly reduced the levels of total protein, inflammatory cells, inflammatory cytokines such as IL-1, IL-6, IL-8, tumour necrosis factor-alpha (TNF-a) and transforming growth factor (TGF). Besides, the histopathological examination of MP infected mice lung tissue showed the cellular arrangements were effectively retained after administration of synthesized ZnO-NPs.

    CONCLUSION: In conclusion, synthesized ZnO-NPs alleviate pneumonia progression via reducing the level of inflammatory cytokines and inflammatory cells in MP infected mice model.

    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis*
  7. An Overview of the Activities of Cefiderocol Against Sensitive and Multidrug- Resistant (MDR) Bacteria
    AlMatar M, Albarri O, Makky EA, Var I, Köksal F
    Mini Rev Med Chem, 2020;20(18):1908-1916.
    PMID: 32811410 DOI: 10.2174/1389557520666200818211405
    The need for new therapeutics and drug delivery systems has become necessary owing to the public health concern associated with the emergence of multidrug-resistant microorganisms. Among the newly discovered therapeutic agents is cefiderocol, which was discovered by Shionogi Company, Japan as an injectable siderophore cephalosporin. Just like the other β-lactam antibiotics, cefiderocol exhibits antibacterial activity via cell wall synthesis inhibition, especially in Gram negative bacteria (GNB); it binds to the penicillin-binding proteins, but its unique attribute is that it crosses the periplasmic space of bacteria owing to its siderophore-like attribute; it also resists the activity of β-lactamases. Among all the synthesized compounds with the modified C-7 side chain, cefiderocol (3) presented the best and well-balanced activity against multi-drug resistant (MDR) Gram negative bacteria, including those that are resistant to carbapenem. İn this article, an overview of the recent studies on cefiderocol was presented.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  8. Anti-acne, anti-dandruff and anti-breast cancer efficacy of green synthesised silver nanoparticles using Coriandrum sativum leaf extract
    Sathishkumar P, Preethi J, Vijayan R, Mohd Yusoff AR, Ameen F, Suresh S, et al.
    J. Photochem. Photobiol. B, Biol., 2016 Oct;163:69-76.
    PMID: 27541567 DOI: 10.1016/j.jphotobiol.2016.08.005
    In this present investigation, AgNPs were green synthesised using Coriandrum sativum leaf extract. The physicochemical properties of AgNPs were characterised using UV-visible spectrophotometer, field emission scanning microscopy/energy dispersive X-ray (FESEM/EDX), Fourier transformed infrared spectroscopy (FT-IR), X-ray diffraction (XRD) and Brunauer-Emmett-Teller (BET) analysis. Further, in vitro anti-acne, anti-dandruff and anti-breast cancer efficacy of green synthesised AgNPs were assessed against Propionibacterium acnes MTCC 1951, Malassezia furfur MTCC 1374 and human breast adenocarcinoma (MCF-7) cell line, respectively. The flavonoids present in the plant extract were responsible for the AgNPs synthesis. The green synthesised nanoparticles size was found to be ≈37nm. The BET analysis result shows that the surface area of the synthesised AgNPs was found to be 33.72m(2)g(-1). The minimal inhibitory concentration (MIC) of AgNPs for acne causative agent P. acnes and dandruff causative agent M. furfur was found to be at 3.1 and 25μgmL(-1), respectively. The half maximal inhibitory concentration (IC50) value of the AgNPs for MCF-7 cells was calculated as 30.5μgmL(-1) and complete inhibition was observed at a concentration of 100μgmL(-1). Finally, our results proved that green synthesised AgNPs using C. sativum have great potential in biomedical applications such as anti-acne, anti-dandruff and anti-breast cancer treatment.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  9. Antibacterial and antioxidant potential of biosynthesized copper nanoparticles mediated through Cissus arnotiana plant extract
    Rajeshkumar S, Menon S, Venkat Kumar S, Tambuwala MM, Bakshi HA, Mehta M, et al.
    J. Photochem. Photobiol. B, Biol., 2019 Aug;197:111531.
    PMID: 31212244 DOI: 10.1016/j.jphotobiol.2019.111531
    Environment friendly methods for the synthesis of copper nanoparticles have become a valuable trend in the current scenario. The utilization of phytochemicals from plant extracts has become a unique technology for the synthesis of nanoparticles, as they possess dual nature of reducing and capping agents to the nanoparticles. In the present investigation we have synthesized copper nanoparticles (CuNPs) using a rare medicinal plant Cissus arnotiana and evaluated their antibacterial activity against gram negative and gram positive bacteria. The morphology and characterization of the synthesized CuNPs were studied and done using UV-Visible spectroscopy at a wavelength range of 350-380 nm. XRD studies were performed for analyzing the crystalline nature; SEM and TEM for evaluating the spherical shape within the size range of 60-90 nm and AFM was performed to check the surface roughness. The biosynthesized CuNPs showed better antibacterial activity against the gram-negative bacteria, E. coli with an inhibition zone of 22.20 ± 0.16 mm at 75 μg/ml. The antioxidant property observed was comparatively equal with the standard antioxidant agent ascorbic acid at a maximum concentration of 40 μg/ ml. This is the first study reported on C. arnotiana mediated biosynthesis of copper nanoparticles, where we believe that the findings can pave way for a new direction in the field of nanotechnology and nanomedicine where there is a significant potential for antibacterial and antioxidant activities. We predict that, these could lead to an exponential increase in the field of biomedical applications, with the utilization of green synthesized CuNPs, due to its remarkable properties. The highest antibacterial property was observed with gram-negative strains mainly, E. coli, due to its thin peptidoglycan layer and electrostatic interactions between the bacterial cell wall and CuNPs surfaces. Hence, CuNPs can be potent therapeutic agents in several biomedical applications, which are yet to be explored in the near future.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  10. Antibacterial efficacy of poly(hexamethylene biguanide) immobilized on chitosan/dye-modified nanofiber membranes
    Xu FX, Ooi CW, Liu BL, Song CP, Chiu CY, Wang CY, et al.
    Int J Biol Macromol, 2021 Jun 30;181:508-520.
    PMID: 33775766 DOI: 10.1016/j.ijbiomac.2021.03.151
    This study aimed to develop a novel electrospun polyacrylonitrile (PAN) nanofiber membrane with the enhanced antibacterial property. The PAN nanofiber membrane was first subjected to alkaline hydrolysis treatment, and the treated membrane was subsequently grafted with chitosan (CS) to obtain a CS-modified nanofiber membrane (P-COOH-CS). The modified membrane was then coupled with different dye molecules to form P-COOH-CS-Dye membranes. Lastly, poly(hexamethylene biguanide) hydrochloride (PHMB) was immobilized on the modified membrane to produce P-COOH-CS-Dye-PHMB. Physical characterization studies were conducted on all the synthesized nanofiber membranes. The antibacterial efficacies of nanofiber membranes prepared under different synthesis conditions were evaluated systematically. Under the optimum synthesis conditions, P-COOH-CS-Dye-PHMB was highly effective in disinfecting a high concentration of Escherichia coli, with an antibacterial efficacy of approximately 100%. Additionally, the P-COOH-CS-Dye-PHMB exhibited an outstanding wash durability as its antibacterial efficacy was only reduced in the range of 5%-7% even after 5 repeated cycles of treatment. Overall, the experimental results of this study suggested that the P-COOH-CS-Dye-PHMB is a promising antibacterial nanofiber membrane that can be adopted in the food, pharmaceutical, and textile industries.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  11. Antibacterial, antifungal and anticonvulsant evaluation of novel newly synthesized 1-[2-(1H-tetrazol-5-yl)ethyl]-1H-benzo[d][1, 2,3]triazoles
    Rajasekaran A, Murugesan S, AnandaRajagopal K
    Arch Pharm Res, 2006 Jul;29(7):535-40.
    PMID: 16903071
    Several novel 1-[2-(1H-tetrazol-5-yl) ethyl]-1H-benzo[d][1,2,3]triazoles (3a-h) have been synthesized by the condensation of 1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-benzotriazole (2) and appropriate acid chlorides. 1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-benzotriazole (2) was synthesized by reacting 3-(1H-benzo[d][1,2,3]triazol-1-yl)propanenitrile with sodium azide and ammonium chloride in the presence of dimethylformamide. The synthesized compounds were characterized by IR and PMR analysis. The titled compounds were evaluated for their in-vitro antibacterial and antifungal activity by the cup plate method and anticonvulsant activity evaluated by the maximal electroshock induced convulsion method in mice. All synthesized compounds exhibited moderate antibacterial activity against Bacillus subtilis and moderate antifungal activity against Candida albicans. Compounds 5-(2-(1H-benzo[d][1,2,3]triazo-1-yl)ethyl)-1H-tetrazol-1-yl)(4-aminophenyl)methanone 3d and 5-(2-(1 H-benzo[d][1,2,3]triazo-1-yl)ethyl)-1H-tetrazol-1-yl)(2-aminophenyl)methanone 3e elicited excellent anticonvulsant activity.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  12. Fulltext Antimicrobial and antioxidant activities of new metal complexes derived from 3-aminocoumarin
    Kadhum AA, Mohamad AB, Al-Amiery AA, Takriff MS
    Molecules, 2011 Aug 15;16(8):6969-84.
    PMID: 21844844 DOI: 10.3390/molecules16086969
    3-Aminocoumarin (L) has been synthesized and used as a ligand for the formation of Cr(III), Ni(II), and Cu(II) complexes. The chemical structures were characterized using different spectroscopic methods. The elemental analyses revealed that the complexes where M=Ni(II) and Cu(II) have the general formulae [ML(2)Cl(2)], while the Cr(III) complex has the formula [CrL(2)Cl(2)]Cl. The molar conductance data reveal that all the metal chelates, except the Cr(III) one, are non-electrolytes. From the magnetic and UV-Visible spectra, it is found that these complexes have octahedral structures. The stability for the prepared complexes was studied theoretically using Density Function Theory. The total energy for the complexes was calculated and it was shown that the copper complex is the most stable one. Complexes were tested against selected types of microbial organisms and showed significant activities. The free radical scavenging activity of metal complexes have been determined by measuring their interaction with the stable free radical DPPH and all the compounds have shown encouraging antioxidant activities.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis*
  13. Antimycobacterial activity: synthesis of novel 3-(substituted phenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues
    Ali MA, Ismail R, Choon TS, Pandian S, Hassan Ansari MZ
    J Enzyme Inhib Med Chem, 2011 Aug;26(4):598-602.
    PMID: 21714764 DOI: 10.3109/14756366.2010.529805
    In this study, a series of novel 3-(substituted phenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues were synthesized and evaluated for antimycobacterial activity against Mycobacterium tuberculosis (MTB) H(37)Rv and isoniazid resistant M. tuberculosis (INHR-MTB). All the newly synthesized compounds were showing moderate to high inhibitory activities. The compound 6,7-dimethoxy-3-(4-chloro phenyl)-4H-indeno[1,2-c]isoxazole (4b) was found to be the most promising compound, active against MTB H(37)Rv and INHR-MTB with minimum inhibitory concentrations of 0.22 and 0.34 μM.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  14. Antimycobacterial evaluation of novel hybrid arylidene thiazolidine-2,4-diones
    Ponnuchamy S, Kanchithalaivan S, Ranjith Kumar R, Ali MA, Choon TS
    Bioorg Med Chem Lett, 2014 Feb 15;24(4):1089-93.
    PMID: 24472146 DOI: 10.1016/j.bmcl.2014.01.007
    A series of novel hybrid heterocycles comprising arylidene thiazolidine-2,4-dione and 1-cyclopropyl-2-(2-fluorophenyl)ethanone were synthesized. These compounds were evaluated for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv in High Throughput Screen. Most of the hybrid arylidene thiazolidine-2,4-diones displayed moderate to good activity with MIC of less than 50 μM. Compound 1m exhibited maximum potency being 5.87 fold more active at EC50 and 6.26 fold more active at EC90 than the standard drug pyrimethamine.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  15. Fulltext Autoclave-assisted synthesis of AgNPs in Z. officinale extract and assessment of their cytotoxicity, antibacterial and antioxidant activities
    Kalantari K, Afifi AM, Moniri M, Moghaddam AB, Kalantari A, Izadiyan Z
    IET Nanobiotechnol, 2019 May;13(3):262-268.
    PMID: 31053688 DOI: 10.1049/iet-nbt.2018.5066
    In this study, the authors synthesised silver nanoparticles (AgNPs) using autoclave as a simple, unique and eco-friendly approach. The effect of Zingiber officinale extract was evaluated as a reducing and stabiliser agent. According to transmission electron microscopy results, the AgNPs were in the spherical shape with a particle size of ∼17 nm. The biomedical properties of AgNPs as antibacterial agents and free radical scavenging activity were estimated. Synthesised AgNPs showed significant 1,1-diphenyl-2-picryl-hydrazyl free radical scavenging. Strong bactericidal activity was shown by the AgNPs on Gram-positive and Gram-negative bacteria. A maximum inhibition zone of ∼14 mm was obtained for epidermidis at a concentration of 60 μg/ml for sample fabricated at 24 h. The AgNPs also showed a significant cytotoxic effect against MCF-7 breast cancer cell lines with an half maximal inhibitory concentration value of 62 μg/ml in 24 h by the MTT assay. It could be concluded that Z. officinale extract can be used effectively in the production of potential antioxidant and antimicrobial AgNPs for commercial application.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis*
  16. BSA Binding, molecular docking and in vitro biological screening of some new 1, 2, 4-triazole heterocycles bearing azinane nucleus
    Iqbal J, Rehman A, Abbasi MA, Siddiqui SZ, Khalid H, Laulloo SJ, et al.
    Pak J Pharm Sci, 2020 Jan;33(1):149-160.
    PMID: 32122843
    A series of new compounds (5a-q), derived from 5-(1-(4-nitrophenylsulfonyl) piperidin-4-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol (3) were proficiently synthesized to evaluate their biological activities. 1-(4-Nitrophenylsulfonyl) piperidine-4-carbohydrazide (2) was refluxed with phenylisothiocyanate to yield an adduct which was cyclized to compound 3 by reflux reaction with 10 % potassium hydroxide. The targeted compounds 5a-q, were synthesized by stirring alkyl/aralkyl halides (4a-q) and compound 3 in a polar aprotic solvent. 1H-NMR, 13C-NMR, EI-MS and IR spectral techniques were employed to confirm the structures of all the synthesized compounds. The compounds were biologically evaluated for BSA binding studies followed by anti-bacterial, anti-inflammatory and acetylcholinesterase (AChE) activities. The active sites responsible for the best AChE inhibition were identified through molecular docking studies. Compound 5e bearing 4-chlorobenzyl moiety found most active antibacterial and anti-inflammatory agent among the synthesized compounds. The whole library of synthesized compounds except compounds 5d and 5f was found highly active for AChE inhibition and recommended for in vivo studies so that their therapeutic applications may come in utilization.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  17. Biogenic approach to synthesize rod shaped Gd2 O3 nanoparticles and its optimization using response surface methodology-Box-Behnken design model
    Surendra TV, Mohana Roopan S, Khan MR
    Biotechnol Prog, 2019 07;35(4):e2823.
    PMID: 31017346 DOI: 10.1002/btpr.2823
    The rare earth metal oxide nanoparticles such as gadolinium oxide nanoparticles (Gd2 O3 NPs) have been synthesized by green synthesis process using methanolic extract of Moringa oleifera (M oleifera) peel. In this process, the Gd2 O3 NPs formation was observed at 280-300 nm in UV-Vis spectroscopy. The XRD pattern of the synthesized Gd2 O3 NPs was exactly matched with JCPDS No 3-065-3181which confirms the crystalline nature of Gd2 O3 NPs. In addition, Energy-dispersive X-ray spectroscopy (EDX) analysis was stated that Gd and O elements were present as 70.31 and 29.69%, respectively in Gd2 O3 NPs. The SEM and TEM analysis were said Gd2 O3 NPs are in rod shape and 26 ± 2 nm in size. Further the synthesized Gd2 O3 NPs were confirmed by X-ray photoemission spectroscopy (XPS). The synthesized Gd2 O3 NPs were further examined for anti-fungal activity against Alternaria saloni (A saloni) and Sclerrotium rolfsii (S rolfsii) and it showed moderate activity. Also, Gd2 O3 NPs evaluated as good antibacterial agent against different Gram +ve and Gram -ve bacteria. Moreover, the toxicity of the Gd2 O3 NPs on red blood cells (RBCs) of the human blood was determined using hemolytic assay, the obtained results were stated the synthesized Gd2 O3 NPs are nontoxic to the human erythrocytes. The photocatalytic activity against malachite green (MG) dye was tested and confirmed as 92% of dye was degraded within 2 hr by Gd2 O3 NPs. The results were stated the green synthesized Gd2 O3 NPs are good anti-fungal agents, nontoxic and we can use as a photocatalyst. Copyright © 2019 John Wiley & Sons, Ltd.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  18. D-glucosamine chitosan base molecule-assisted synthesis of different shape and sized silver nanoparticles by a single pot method: A greener approach for sensor and microbial applications
    Ranjani B, Pandian K, Kumar GA, Gopinath SCB
    Int J Biol Macromol, 2019 Jul 15;133:1280-1287.
    PMID: 31051204 DOI: 10.1016/j.ijbiomac.2019.04.196
    Silver nanoparticle was synthesized using D-glucosamine chitosan base as green reducing agent at elevated temperature in alkaline pH ranges. The excess of D-glucosamine chitosan base was used as it is both stabilizing and reducing agent at different pHs, regulates the shape and size of the silver nanoparticles. The progressive growth of silver nanoparticles was monitored by UV-Visible spectral studies. A sharp peak at 420 nm indicates the formation of spherical silver nanoparticles. The size and shape of silver nanoparticles were observed from Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM) methods. The anisotropically grown nanoparticles were used as probe for Surface Enhanced Raman Studies (SERS) using ATP (4-aminothiophenol) as a model system. The catalytic behavior of silver nanoparticles was exploited for 4-nitrophenol reduction and observed that the reduction reaction follows pseudo first order kinetics with a rate constant 0.65 min. The antibacterial activity of silver nanoparticles was also tested for both gram-positive and -negative microorganisms, in which higher zone of inhibition was observed for gram negative microorganism.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis*
  19. Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives
    Mohammed AAM, Suaifan GARY, Shehadeh MB, Okechukwu PN
    Eur J Med Chem, 2020 Sep 15;202:112513.
    PMID: 32623216 DOI: 10.1016/j.ejmech.2020.112513
    Herein we report the design, synthesis and biological evaluation of structurally modified ciprofloxacin, norfloxacin and moxifloxacin standard drugs, featuring amide functional groups at C-3 of the fluoroquinolone scaffold. In vitro antimicrobial testing against various Gram-positive bacteria, Gram-negative bacteria and fungi revealed potential antibacterial and antifungal activity. Hybrid compounds 9 (MIC 0.2668 ± 0.0001 mM), 10 (MIC 0.1358 ± 00025 mM) and 13 (MIC 0.0898 ± 0.0014 mM) had potential antimicrobial activity against a fluoroquinolone-resistant Escherichia coli clinical isolate, compared to ciprofloxacin (MIC 0.5098 ± 0.0024 mM) and norfloxacin (MIC 0.2937 ± 0.0021 mM) standard drugs. Interestingly, compound 10 also exerted potential antifungal activity against Candida albicans (MIC 0.0056 ± 0.0014 mM) and Penicillium chrysogenum (MIC 0.0453 ± 0.0156 mM). Novel derivatives and standard fluoroquinolone drugs exhibited near-identical cytotoxicity levels against L6 muscle cell-line, when measured using the MTT assay.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis
  20. Fulltext Efficient Catalyst One-Pot Synthesis of 7-(Aryl)-10,10-dimethyl-10,11-dihydrochromeno[4,3-b]chromene-6,8(7H,9H)-dione Derivatives Complemented by Antibacterial Activity
    Al-Majedy YK, Al-Amiery AA, Kadhum AA, Mohamad AB
    Biomed Res Int, 2016;2016:5891703.
    PMID: 27563671 DOI: 10.1155/2016/5891703
    The problem of bacteria resistance to many known agents has inspired scientists and researchers to discover novel efficient antibacterial drugs. Three rapid, clean, and highly efficient methods were developed for one-pot synthesis of 7-(aryl)-10,10-dimethyl-10,11-dihydrochromeno[4,3-b]chromene-6,8(7H,9H)-dione derivatives. Three components are condensed in the synthesis, 4-hydroxycoumarin, 5,5-dimethyl-1,3-cyclohexanedione, and aromatic aldehydes, using tetrabutylammonium bromide (TBAB), diammonium hydrogen phosphate (DAHP), or ferric chloride (FeCl3), respectively. Each method has different reaction mechanisms according to the catalyst. The present methods have advantages, including one-pot synthesis, excellent yields, short reaction times, and easy isolation of product. All catalysts utilized in our study could be reused several times without losing their catalytic efficiency. All synthesized compounds were fully characterized and evaluated for their antibacterial activity.
    Matched MeSH terms: Anti-Bacterial Agents/chemical synthesis*
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