scholarly journals Antibacterial and Anticancer Properties of New Fluoroquinolones

2019 ◽  
Vol 32 (2) ◽  
pp. 427-434
Author(s):  
Maha R. Al Rimawi ◽  
Yusuf M. Al-Hiari ◽  
Amal G. Al-Bakri ◽  
Sanaa K. Bardaweel
Keyword(s):  
Antibacterial Agents ◽  
Spectroscopic Techniques ◽  
Cell Culture System ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Anticancer Properties ◽  
Gram Positive Bacteria ◽  
Good Antibacterial Activity ◽  
Weak Activity

Fluoroquinolones are clinically successful antibacterial agents. In this work a series of novel 7-substituted anilino-8-nitrofluoroquinolone esters (3-9), acids (10-16) and 8-amino reduced derivatives (17-23) of the later compounds were successfully prepared and characterized using spectroscopic techniques. All the compounds tested (10-23) showed good antibacterial activity against both Gram-positive and Gram- negative standard bacterial strains. Interestingly, 8-amino reduced derivatives (17-22) were more active against both standard strains than their 8-nitro acid analogues (10-15). Moreover, some targeted compounds have shown reasonable activity mainly against resistant gram positive bacteria. In particular compounds 10, 12 and 16 displayed a potent activity against methicillin resistant S. aureus (MRSA) with MIC values of 4.7, 2.3 and 1.2 μg/mL, respectively. Lipophilicity could be a plausible explanation of such higher activity against the gram positive resistant strain (MRSA). Biological screening of cytotoxic activity against five cancer cell lines using an in vitro cell culture system was achieved for all tested compounds. These derivatives have shown weak activity for most of them. Interestingly, more lipophilic nitroacids (10-15) were more active than their analogous reduced acids (17-22).

scholarly journals Phytochemical analyses and antibacterial activities of Erodium, Euphorbia, Logoecia and Tamarix species

2019 ◽  
Vol 13 (11) ◽  
pp. 1013-1020
Author(s):  
Khaldoun J Al-Hadid ◽  
Nehaya Al-Karablieh ◽  
Ahmad Sharab ◽  
Ihsan Mutlak
Keyword(s):  
Antibacterial Agents ◽  
Antibacterial Activities ◽  
Microtiter Plate ◽  
Phytochemical Analysis ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Phytochemical Components ◽  
Promising Source ◽  
Group D

Introduction: Resistance against commonly used antibacterial agents has become a globally recognized threat to human health. Therefore, the development of new and effective antibacterial agents is necessary to treat infections caused by resistant bacterial strains; plants are a promising source of new agents to be tested. Methodology: The minimum inhibitory concentrations (MIC) of ethanolic extracts of Erodium gruinum, Euphorbia hierosolymitana, Logoecia cuminoides, and Tamarix tetragyna against 10 Gram-negative and 5 Gram-positive bacteria were determined using agar well diffusion and microtiter plate dilution methods, respectively. The phytochemical composition of the crude extracts of the plants was determined using HPLC. Results: Pseudomonas aeruginosa ATCC 27853, Klebsiella pneumoniae, Proteus mirabilis, and Acinetobacter baumannii were sensitive to E. gruinum and E. hierosolymitana extracts. P. aeruginosa ATCC 27853 and M. catarrhalis were sensitive to L. cuminoides extract. P. aeruginosa ATCC 27853, P. mirabilis, and K. pneumoniae were sensitive to T. tetragyna extracts. For Gram-positive bacteria, Staphylococcus aureus ATCC 33591 and ATCC 43300 were sensitive to E. gruinum and E. hierosolymitana extracts. S. aureus ATCC 43300 and ATCC 33591 and Group D Streptococcus were sensitive to T. tetragyna extract. All Gram-positive bacteria were completely resistant to the extract of L. cuminoides. The major phytochemical components of the plant extracts belonged to flavonoids, tannins, terpenes, quinones, phytosterols, phytoestrogens, carbohydrates, fatty acids, and coumarin. Conclusion: The study showed the potential of the development of antibacterial agents from these plants. Phytochemical analysis revealed compounds that are candidates for new antibacterial drugs.

scholarly journals Synthesis and Pharmacological Evaluation of Some New 2-Phenyl benzimidazoles Derivatives and their Schiff's Bases

2009 ◽  
Vol 6 (s1) ◽  
pp. S342-S346 ◽  
Author(s):  
Y. S. Chhonker ◽  
B. Veenu ◽  
S. R. Hasim ◽  
Niranjan Kaushik ◽  
Devendra Kumar ◽  
...  
Keyword(s):  
Antimicrobial Activities ◽  
Benzimidazole Derivatives ◽  
Spectroscopic Techniques ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Ir Spectroscopic

Some new 2- phenyl benzimidazole derivatives were synthesised by cyclocondensation with appropriate reagents. The compounds synthesised were identified by1H NMR, FAB Mass and FT-IR spectroscopic techniques. All compounds studied in this work were screened for theirin vitroantimicrobial activities against the standard strains:Staphylococcus aureusATCC - 25923, ATCC - 441 andBacillus subtilisATCC- 6633 as gram positive,Escherichia coliATCC - 11775 andPseudomonas aeruginosaATCC 10145 as gram negative bacteria. Some of the compounds inhibited the growth of gram-positive bacteria (B. subtilisandS. aureus) at MIC values between 25 and 200 mg/mL. Some of the compounds exhibit antimicrobial activity against gram negative bacteria (E. coliandP. Aeruginosa) MIC values between 25 and 200 mg/mL.

scholarly journals Design, synthesis and molecular modeling study of substituted indoline-2-ones and spiro[indole-heterocycles] with potential activity against Gram-positive bacteria

2021 ◽  
Vol 72 (1) ◽  
pp. 79-95
Author(s):  
Awwad Abdoh Radwan ◽  
Fares Kaed Aanazi ◽  
Mohammed Al-Agamy ◽  
Gamal Mohammad Mahrous
Keyword(s):  
Histidine Kinase ◽  
In Silico ◽  
Binding Mode ◽  
Antibacterial Activities ◽  
Hydroxy Ketone ◽  
Spectroscopic Techniques ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Chemical Structures

Abstract Longstanding and firsthand infectious diseases are challenging community health threats. A new series of isatin derivatives bearing β-hydroxy ketone, chalcone, or spiro-heterocycle moiety, was synthesized in a good yield. Chemical structures of the synthesized compounds were elucidated using spectroscopic techniques and elemental analysis. Antibacterial activities of the compounds were then evaluated in vitro and by in silico modeling. The compounds were more active against Gram-positive bacteria, Staphylococcus aureus (MIC = 0.026–0.226 mmol L−1) and Bacillus subtilis (MIC = 0.348–1.723 mmol L–1) than against Gram-negative bacteria (MIC = 0.817–7.393 mmol L–1). Only 3-hydroxy-3-(2-(2,5-dimethylthiophen-3-yl)-2-oxoethyl)indolin-2-one (1b) was found as active as imipenem against S. aureus (MIC = 0.026 mmol L–1). In silico docking of the compounds in the binding sites of a homology modeled structure of S. aureus histidine kinase-Walk allowed us to shed light on the binding mode of these novel inhibitors. The highest antibacterial activity of 1b is consistent with its highest docking score values against S. aureus histidine kinase.

scholarly journals Synthesis, characterization, and in vitro antimicrobial investigation of novel pyran derivatives based on 8-hydroxyquinoline

2019 ◽  
Vol 8 (1) ◽  
Author(s):  
Mohamed Rbaa ◽  
Abdelhadi Hichar ◽  
Omar Bazdi ◽  
Younes Lakhrissi ◽  
Khadija Ounine ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Magnetic Resonance ◽  
Penicillin G ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Wide Range

Abstract Background 8-Hydroxyquinoline derivatives are known for their extensive applications in the field of analytical chemistry and separation techniques; their complexes with transition metals also exhibit antibacterial and antifungal activity. Results In the present study, we synthesized a new series of pyranoquinoline derivatives and evaluated their antibacterial activities. The structures of the synthesized compounds were characterized by Fourier transform infrared (FT-IR), hydrogen-1 nuclear magnetic resonance, carbon-13 nuclear magnetic resonance, and elemental analysis. All the prepared compounds were evaluated in vitro as antimicrobial agents against Gram-positive and Gram-negative bacterial strains (Escherichia coli (ATCC35218), Staphylococcus aureus (ATCC29213), Vibrio parahaemolyticus (ATCC17802), and Pseudomonas aeruginosa (ATCC27853)). The screening test was determined by using the standard protocol of disc diffusion method (DDM). Conclusion We have synthesized new pyranic compounds bearing an 8-hydroxyquinoline moiety on their structure. The preliminary screening results showed that all the tested compounds have a remarkable inhibitory effect on the growth of the majority of the tested bacterial strains compared to the standard antibiotic (penicillin G), and the chlorinated compound (Q1) is more active against Gram-positive bacteria than Gram-negative bacteria such as the Staphylococcus aureus strain which is the most sensitive. Gram-positive bacteria are responsible for a wide range of infectious diseases, and rising resistance in this group is causing increasing concern. Thus, this study develops novel heterocyclic compound derivatives of 8-hydroxyquinoline that have demonstrated good antibacterial activity against Gram-positive bacteria. Graphical abstract

scholarly journals The Biological Evaluation of Fusidic Acid and Its Hydrogenation Derivative as Antimicrobial and Anti-inflammatory Agents

2018 ◽  
Author(s):  
Pan-Pan Wu ◽  
Hao He ◽  
W. David Hong ◽  
Tong-Rong Wu ◽  
Su-Qing Zhao ◽  
...  
Keyword(s):  
Fusidic Acid ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Ear Edema ◽  
Gram Positive Bacteria ◽  
Mouse Ear ◽  
Anti Inflammatory

AbstractFusidic acid (WU-FA-00) is the only commercially available antimicrobial from the fusidane family that has a narrow spectrum of activity against Gram-positive bacteria. Herein, the hydrogenation derivative (WU-FA-01) of fusidic acid was prepared, and both compounds were examined against a panel of six bacterial strains. In addition, their anti-inflammation properties were evaluated using a 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema model. The results of the antimicrobial assay revealed that both WU-FA-00 and WU-FA-01 displayed a high level of antimicrobial activity against Gram-positive strains. Moreover, killing kinetic studies were performed, and the results were in accordance with the MIC and MBC results. We also demonstrated that the topical application of WU-FA-00 and WU-FA-01 effectively decreased TPA-induced ear edema in a dose-dependent manner. This inhibitory effect was associated with the inhibition of TPA-induced up-regulation of pro-inflammation cytokines IL-1β, TNF-α and COX-2. WU-FA-01 significantly suppressed the expression levels of p65, IκB-α, and p-IκB-α in the TPA-induced mouse ear model. Overall, our results showed that WU-FA-00 and WU-FA-01 not only had effective antimicrobial activitiesin vitro, especially to the Gram-positive bacteria, but also possessed strong anti-inflammatory effectsin vivo. These results provide a scientific basis for developing fusidic acid derivatives as antimicrobial and anti-inflammatory agents.

scholarly journals Chemical Composition and Antibacterial Activity of Rhizome Oils from Five Hedychium Species

2013 ◽  
Vol 8 (4) ◽  
pp. 1934578X1300800
Author(s):  
Ratchuporn Suksathan ◽  
Siriwoot Sookkhee ◽  
Somboon Anuntalabhochai ◽  
Sunee Chansakaow
Keyword(s):  
Antibacterial Activity ◽  
Chemical Composition ◽  
Essential Oils ◽  
Inhibition Zone ◽  
Bacterial Strains ◽  
Capillary Gc ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Weak Activity ◽  
Bacteria Inhibition

The essential oils from rhizomes of five Hedychium species, H. coronarium, H. neocarneum, H. flavescens, H. speciosum and H. stenopetalum (Zingiberaceae), were obtained by hydrodistillation and analyzed by capillary GC and GC/MS. Sixty components were identified and percentage oil yields from the fresh plants ranged from 0.06-0.17 % (v/w). All rhizome oils were rich in terpenes, especially monoterpenes (75.0-95.9 %). The most common compounds in the rhizome oils of Hedychium were β-pinene, linalool and 1,8-cineole. The essential oils were tested against four bacterial strains. They showed moderate to weak activity against Gram-positive bacteria (inhibition zone 25-13 mm, MIC 0.3-8.3 mg/mL, MBC 0.6-8.3 mg/mL).

scholarly journals In Vitro Activities of Linezolid against Important Gram-Positive Bacterial Pathogens Including Vancomycin-Resistant Enterococci

1999 ◽  
Vol 43 (8) ◽  
pp. 2059-2062 ◽  
Author(s):  
Gary A. Noskin ◽  
Farida Siddiqui ◽  
Valentina Stosor ◽  
Donna Hacek ◽  
Lance R. Peterson
Keyword(s):  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Active Agent ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
New Class ◽  
Vancomycin Resistant Enterococci ◽  
Vancomycin Resistant ◽  
Emergence Of Resistance

ABSTRACT The emergence of resistance in gram-positive bacteria has necessitated a search for new antimicrobial agents. Linezolid is an oxazolidinone, a new class of antibacterial agents with enhanced activity against pathogens. We compared the activity of linezolid to those of other antimicrobial agents against 3,945 clinical isolates. Linezolid demonstrated potent activity against all isolates tested. For all vancomycin-susceptible enterococci, staphylococci, and streptococci, the activity of linezolid was comparable to that of vancomycin. Against oxacillin-resistant staphylococci and vancomycin-resistant enterococci, linezolid was the most active agent tested. In summary, linezolid appears to be a promising new antimicrobial agent for the treatment of gram-positive infections.

Skuteczność działania in vitro olejku melisowego (Oleum Melissae) na bakterie beztlenowe

2019 ◽  
Vol 20 (4) ◽  
Author(s):  
Anna Kędzia ◽  
Elżbieta Hołderna-Kędzia
Keyword(s):  
Essential Oil ◽  
Anaerobic Bacteria ◽  
Growth Control ◽  
Geranyl Acetate ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
High Antibacterial Activity

Introduction. Melissa officinalis L. is a member of family Lamiaceae. The plant a widely cultivated in many countries of Asia (Iran, Turkiestan), North America, Europe and Poland. It growth to 1 m high. Leaves are green with characteristic smell of lemon and flowers are white or pink. The plant produce of essential oil which the components are: neral, geraniol, geranial, β-caryophyllene, tymol, linalol, citronellol, cytronellal, geranyl acetate, α-humulene, germacrane D, n-eikosane, didydrocitronellolacetate, 5-cedranone, β-ocimene Z and β-ocimene E. The oil is used in therapy. It showed antiinflammatory and antymicrobial activity towards bacteria, fungi, viruses and insects. Aim. The aim of this study was to evaluate the activity of melissa oil against anaerobic bacteria. Material and methods. The bacterial strains were isolated from oral cavity. A total 32 strains anaerobes and 8 standards strains were investigated. The melissa oil (Semifarm) was dissolved in DMSO and distilled water to obtained a final concentrations of 2.0, 1.0, 0.5, 0.25, 0.12 and 0.06 mg/ml. The inoculums containing 105 CFU/spot was seeded with Steers replicator upon the surface of agar with or without essential oil (bacterial strains growth control). Incubation was performed in anaerobic conditions in anaerobic jar, in 37°C for 48 hrs. The MIC was defined as the lowest concentrations of melissa oil inhibiting the growth of the tested anaerobes. Results. The results showed, that the melissa oil presented high antibacterial activity against all tested anaerobes. The most susceptible from Gram-positive bacteria were the cocci from the genus of Finegoldia magna, Micromonas micros and Peptostreptococcus anaerobius and Gram-positive rods Actinomyces odontolyticus and Bifidobacterium bivia (MIC < 0.06 mg/ml). The 92% of Gram-positive bacteria was inhibited in concentrations < 0.06-0.25 mg/ml. From Gram-negative rods the most susceptible was the Bacteroides vulgatus (MIC < 0.06 mg/ml). The strains from genus of Prevotella bivia and Prevotella buccalis were the lowest sensitive. The minimal inhibitory concentration for these strains was 1.0 mg/ml. But 47% of this strains was inhibited by concentrations in range < 0.06-0.25 mg/ml. Conclusions. The melissa oil showed high activity against all tested anaerobic bacteria, The Gram-positive bacteria were the most susceptible to tested oil than Gram-negative anaerobic rods.

scholarly journals Synthesis, characterization, and pharmacological evaluation of thiourea derivatives

2020 ◽  
Vol 18 (1) ◽  
pp. 764-777
Author(s):  
Sumaira Naz ◽  
Muhammad Zahoor ◽  
Muhammad Naveed Umar ◽  
Saad Alghamdi ◽  
Muhammad Umar Khayam Sahibzada ◽  
...  
Keyword(s):  
Spectroscopic Techniques ◽  
Organosulfur Compounds ◽  
Bacterial Strains ◽  
Thiourea Derivatives ◽  
Toxicological Effects ◽  
Pharmaceutical Industries ◽  
Uv Visible ◽  
Hematological And Biochemical Parameters

AbstractThioureas and their derivatives are organosulfur compounds having applications in numerous fields such as organic synthesis and pharmaceutical industries. Symmetric thiourea derivatives were synthesized by the reaction of various anilines with CS2. The synthesized compounds were characterized using the UV-visible and nuclear magnetic resonance (NMR) spectroscopic techniques. The compounds were screened for in vitro inhibition of α-amylase, α-glucosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BuChE) enzymes and for their antibacterial and antioxidant potentials. These compounds were fed to Swiss male albino mice to evaluate their toxicological effects and potential to inhibit glucose-6-phosphatase (G6Pase) inhibition. The antibacterial studies revealed that compound 4 was more active against the selected bacterial strains. Compound 1 was more active against 2,2-diphenyl-1-picrylhydrazyl and 2,2’-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radicals, AChE, BuChE, and α-glucosidase. Compound 2 was more potent against α-amylase and G6Pase. Toxicity studies showed that compound 4 is safe as it exerted no toxic effect on any of the hematological and biochemical parameters or on liver histology of the experimental animals at any studied dose rate. The synthesized compounds showed promising antibacterial and antioxidant potential and were very active (both in vitro and in vivo) against G6Pase and moderately active against the other selected enzymes used in this study.

scholarly journals Silver Nanoparticles and Their Antibacterial Applications

2021 ◽  
Vol 22 (13) ◽  
pp. 7202
Author(s):  
Tamara Bruna ◽  
Francisca Maldonado-Bravo ◽  
Paul Jara ◽  
Nelson Caro
Keyword(s):  
Silver Nanoparticles ◽  
Antibacterial Agents ◽  
Multidrug Resistant ◽  
Secondary Effects ◽  
Cytotoxic Effects ◽  
Factors Affecting ◽  
Gram Positive Bacteria ◽  
Resistant Strains

Silver nanoparticles (AgNPs) have been imposed as an excellent antimicrobial agent being able to combat bacteria in vitro and in vivo causing infections. The antibacterial capacity of AgNPs covers Gram-negative and Gram-positive bacteria, including multidrug resistant strains. AgNPs exhibit multiple and simultaneous mechanisms of action and in combination with antibacterial agents as organic compounds or antibiotics it has shown synergistic effect against pathogens bacteria such as Escherichia coli and Staphylococcus aureus. The characteristics of silver nanoparticles make them suitable for their application in medical and healthcare products where they may treat infections or prevent them efficiently. With the urgent need for new efficient antibacterial agents, this review aims to establish factors affecting antibacterial and cytotoxic effects of silver nanoparticles, as well as to expose the advantages of using AgNPs as new antibacterial agents in combination with antibiotic, which will reduce the dosage needed and prevent secondary effects associated to both.

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