scholarly journals Densely Functionalized 2-methylideneazetidines: Evaluation as Antibacterials

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3891
Author(s):  
Giovanni Petrillo ◽  
Cinzia Tavani ◽  
Lara Bianchi ◽  
Alice Benzi ◽  
Maria Maddalena Cavalluzzi ◽  
...  
Keyword(s):  
Antibacterial Agents ◽  
Inhibitory Concentration ◽  
General Procedure ◽  
Eukaryotic Cells ◽  
Gram Negative Bacteria ◽  
Pharmacological Profile ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Structure Activity

Twenty-two novel, variously substituted nitroazetidines were designed as both sulfonamide and urethane vinylogs possibly endowed with antimicrobial activity. The compounds under study were obtained following a general procedure recently developed, starting from 4-nitropentadienoates deriving from a common β-nitrothiophenic precursor. While being devoid of any activity against fungi and Gram-negative bacteria, most of the title compounds performed as potent antibacterial agents on Gram-positive bacteria (E. faecalis and three strains of S. aureus), with the most potent congener being the 1-(4-chlorobenzyl)-3-nitro-4-(p-tolyl)azetidine 22, which displayed potency close to that of norfloxacin, the reference antibiotic (minimum inhibitory concentration values 4 and 1–2 μg/mL, respectively). Since 22 combines a relatively efficient activity against Gram-positive bacteria and a cytotoxicity on eucharyotic cells only at 4-times higher concentrations (inhibiting concentration on 50% of the cultured eukaryotic cells: 36 ± 10 μM, MIC: 8.6 μM), it may be considered as a promising hit compound for the development of a new series of antibacterials selectively active on Gram-positive pathogens. The relatively concise synthetic route described herein, based on widely available starting materials, could feed further structure–activity relationship studies, thus allowing for the fine investigation and optimization of the toxico-pharmacological profile.

SYNTHESIS OF PIPERINE - PIPERAZINE ANALOGUES AND THEIR ANTIBACTERIAL ACTIVITY

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (06) ◽  
pp. 30-35
Author(s):  
Naveen K. Kottakki ◽  
◽  
Amperayani K. Rao ◽  
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Concentration ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Aromatic Nitro ◽  
Heterocyclic Moiety ◽  
Agar Well Diffusion Method

In the current study, a series of piperine – piperazine analogues (5a to 5f) were designed and synthesized. The piperine was isolated from pepper and used for the conjugation with heterocyclic moiety for better biological activity. The piperazine heterocyclic was chosen for conjugation with piperine. The newly synthesized structures were determined by IR, 1H NMR and 13C NMR spectral data. The compounds were examined for their anti‐microbial activity against gram-positive (Bacillus subtilis) and gram-negative (Vibrio cholerae) bacteria using the agar well diffusion method. The newly synthesized compounds exhibited capable activities against V. cholerae and B. subtilis and it showed minimum inhibitory concentration. Among all the synthesized compounds, 5f has the highest activity (26 mm) against gram-positive bacteria and (29mm) against gram-negative bacteria. The remaining compounds showed appreciable antibacterial activity. The enhanced activity of the synthesized compounds may be due to the presence of conjugated amide linkage with the natural product piperine and piperazine heterocyclic molecule. The substituents present on the aromatic (nitro-substituted) ring also influenced the activity of the compound.

scholarly journals PAMAM-dendrimer Enhanced Antibacterial Effect of Vancomycin Hydrochloride Against Gram-Negative Bacteria

2018 ◽  
Vol 22 ◽  
pp. 10-21 ◽  
Author(s):  
Azadeh Serri ◽  
Arash Mahboubi ◽  
Afshin Zarghi ◽  
Hamid Reza Moghimi
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Concentration ◽  
In Vitro Release ◽  
Pamam Dendrimers ◽  
Dilution Method ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Bacterial Membranes ◽  
Gram Positive Bacteria

Purpose: The antibacterial activity of some antibiotics is specific to either Gram-positive or Gram-negative bacteria.  There are different mechanisms behind such insensitivities like inability of antibiotics to permeate through some bacterial membranes, as is the case for vancomycin in Gram-negative bacteria. The present investigation tries to overcome this problem by dendrimers, in order to make Gram-negative bacteria responsive to vancomycin. Methods: The effects of generations 3 (G3) and 5 (G5) polyamidoamine amine-terminated dendrimers (NH2-PAMAM), on the antibacterial activity of vancomycin, were evaluated. Vancomycin-PAMAM dendrimers complexes were prepared and their antibacterial activities were evaluated by determination of their “minimum inhibitory concentration (MIC)”, “minimum bactericidal concentration” and “fractional inhibitory concentration index” values against two Gram-positive and four Gram-negative bacteria, using broth micro-dilution method. The complexation of vancomycin and dendrimers was also assessed by in vitro release studies across dialysis tubing using a developed HPLC method. Results: Results showed that vancomycin solution was effective against Gram-positive bacteria, but, was not effective in Gram-negative ones. Vancomycin-PAMAM dendrimers exhibited significant antibacterial efficacy against Gram-negative bacteria resulting in a decline of vancomycin MIC values by about 2, 2, 4 and 64 times in E. coli, K. pneumonia, S. typhimurium and P. aeruginosa, respectively. Results also showed that enhanced effect by G5 is more than G3. Dendrimers did not affect antibacterial activity of vancomycin in Gram-positive bacteria, as no permeation problem exists here. Conclusions: The present study revealed that both G3 and G5 cationic PAMAM dendrimers are able to make Gram-negative bacteria sensitive to vancomycin, resulting in decline of MIC values up to 64 times, possibly by increasing its permeation through bacterial membrane. These results look promising for broadening the antibacterial spectrum of vancomycin and such a strategy might be used for increasing the overall life of antibiotics.

scholarly journals Synthesis and Antibacterial Screening of Some 1-Aroyl-3-aryl Thiourea Derivatives

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Love Kumar Soni ◽  
Tamanna Narsinghani ◽  
Rica Jain
Keyword(s):  
Antibacterial Activity ◽  
Gram Negative Bacteria ◽  
Electronic Factor ◽  
Gram Positive ◽  
Thiourea Derivatives ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Antibacterial Screening ◽  
Structure Activity ◽  
Preliminary Study

A series of 1-aroyl-3-aryl thioureas derivatives were synthesized and evaluated for antibacterial activity. The results indicated that the compounds possessed higher activity against gram-negative bacteria than gram-positive bacteria. Amongst all these compounds, C18 (89.4%) exhibited the greatest antibacterial activity against gram-negative bacteria while C5 (85.6%) displayed maximum antibacterial activity against gram-positive bacteria. Preliminary study of the structure-activity relationship revealed that an electronic factor on aryl rings had a great effect on the antibacterial activity of these compounds.

Rapid demonstration of septic or infectious arthritis due to Gram-negative bacteria

1992 ◽  
Vol 50 (1) ◽  
pp. 686-687
Author(s):  
Jacob S. Hanker ◽  
Paul R. Gross ◽  
Beverly L. Giammara
Keyword(s):  
Chronic Arthritis ◽  
Blood Cultures ◽  
Gram Negative Bacteria ◽  
Infectious Arthritis ◽  
Bacterial Arthritis ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria

Blood cultures are positive in approximately only 50 per cent of the patients with nongonococcal bacterial infectious arthritis and about 20 per cent of those with gonococcal arthritis. But the concept that gram-negative bacteria could be involved even in chronic arthritis is well-supported. Gram stains are more definitive in staphylococcal arthritis caused by gram-positive bacteria than in bacterial arthritis due to gram-negative bacteria. In the latter situation where gram-negative bacilli are the problem, Gram stains are helpful for 50% of the patients; they are only helpful for 25% of the patients, however, where gram-negative gonococci are the problem. In arthritis due to gram-positive Staphylococci. Gramstained smears are positive for 75% of the patients.

Antibacterial activity of magnesium oxide nanoparticles prepared by Calcination method

2019 ◽  
Vol 10 (03) ◽  
Author(s):  
Elaf Ayad Kadhem ◽  
Miaad Hamzah Zghair ◽  
Sarah , Hussam H. Tizkam, Shoeb Alahmad Salih Mahdi ◽  
Hussam H. Tizkam ◽  
Shoeb Alahmad
Keyword(s):  
Antibacterial Activity ◽  
Magnesium Oxide ◽  
Diffusion Method ◽  
Oxide Nanoparticles ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Magnesium Oxide Nanoparticles ◽  
Agar Disc

magnesium oxide nanoparticles (MgO NPs) were prepared by simple wet chemical method using different calcination temperatures. The prepared NPs were characterized by Electrostatic Discharge (ESD), Scanning Electron Microscope (SEM) and X-ray Diffraction (XRD). It demonstrates sharp intensive peak with the increase of crystallinty and increase of the size with varying morphologies with respect to increase of calcination temperature. Antibacterial studies were done on gram negative bacteria (E.coli) and gram positive bacteria (S.aureus) by agar disc diffusion method. The zones of inhibitions were found larger for gram positive bacteria than gram negative bacteria, this mean, antibacterial MgO NPs activity more active on gram positive bacteria than gram negative bacteria because of the structural differences. It was found that antibacterial activity of MgO NPs was found it has directly proportional with their concentration.

BAKTERI PADA KARANG SCLERACTINIA DI KAWASAN PERAIRAN BUNAKEN, MOROTAI DAN RAJA AMPAT

2020 ◽  
Vol 8 (1) ◽  
pp. 122
Author(s):  
Eghbert Eghbert Elvan Eghbert Elvan Ampou ◽  
Iis Iis Triyulianti ◽  
Nuryani Widagti ◽  
Suciadi Catur Nugroho ◽  
Yuli Pancawati
Keyword(s):  
Scleractinian Coral ◽  
Gram Negative Bacteria ◽  
Hard Coral ◽  
Field Sampling ◽  
Bacterial Isolation ◽  
Gram Positive ◽  
Coral Mucus ◽  
Gram Negative ◽  
Gram Positive Bacteria

Research on hard coral (Scleractinian coral) contaminated with bacteria is still not much done, especially in Indonesian waters. This study took samples of coral mucus in 2010 at 3 (three) different locations, namely Bunaken (May); Morotai (September) and Raja Ampat (November), which focused on the analysis of Research on hard coral (Scleractinian coral) contaminated with bacteria is still not much done, especially in Indonesian waters. This study took samples of coral mucus in 2010 at 3 (three) different locations, namely Bunaken (May); Morotai (September) and Raja Ampat (November), which focused on the analysis of gram-positive and gram-negative bacteria. The method used for field sampling is time swim, which is by diving at a depth of 5-10 meters for ± 30 minutes and randomly taking samples of coral mucus using siring or by taking directly on corals (reef branching). Mucus samples were analyzed by bacterial isolation in the laboratory. The result shows that there were differences between gram-positive and gram-negative bacteria in the three research sites and that gram-positive bacteria were higher or dominant. Further research that can identify the bacteria species and explain its relationship to the ecosystem is highly recommended.Keywords: Bacteria, Scleractinian coral, gram-positive and -negative, Bunaken, Morotai, Raja Ampat  AbstrakPenelitian tentang karang keras (Scleractinian coral) yang terkontaminasi bakteri masih belum banyak dilakukan, terutama di perairan Indonesia. Penelitian ini mengambil sampel mucus karang pada tahun 2010 di 3 (tiga) lokasi berbeda, yakni Bunaken (Mei); Morotai (September) dan Raja Ampat (November), yang difokuskan pada analisis bakteri gram postif dan gram negatif. Metode yang digunakan untuk pengambilan sampel di lapangan adalah time swim, yaitu dengan penyelaman pada kedalaman 5-10 meter selama ±30 menit dan mengambil sampel mucus karang secara acak menggunakan siring atau dengan mengambil langsung pada karang (fraksi cabang). Sampel mucus dianalisis dengan cara isolasi bakteri di laboratorium. Hasil analisis menunjukkan bahwa ada perbedaan antara bakteri gram positif dan gram negative di tiga lokasi survei dan bakteri gram positif lebih tinggi atau dominan. Penelitian lebih lanjut yang dapat menentukan jenis bakteri serta menjelaskan hubungannya dengan ekosistem sangat disarankan untuk dilakukan.Kata Kunci : Bakteri, Scleractinian coral, gram positif dan negatif, Bunaken, Morotai, Raja Ampat

Structure-Activity Relationship and Antimicrobial Evaluation of N-Phenylpyrazole Curcumin Derivatives

2020 ◽  
Vol 16 (4) ◽  
pp. 481-488
Author(s):  
Heli Sanghvi ◽  
Satyendra Mishra
Keyword(s):  
Antibacterial Activity ◽  
Gram Negative Bacteria ◽  
Pyrazole Derivatives ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Curcumin Derivatives ◽  
Structure Activity ◽  
Electron Donating Groups ◽  
Derivatives Of

Background: Curcumin, one of the most important pharmacologically significant natural products, has gained significant consideration among scientists for decades since its multipharmacological activities. 1, 3-Dicarbonyl moiety of curcumin was found to be accountable for the rapid degradation of curcumin molecule. The aim of present work is to replace 1, 3-dicarbonyl moiety of curcumin by pyrazole and phenylpyrazole derivatives with a view to improving its stability and to investigate the role of substitution in N-phenylpyrazole curcumin on its antibacterial activity against both Gram-positive as well as Gram-negative bacteria. Methods: Pyrazole derivatives of curcumin were prepared by heating curcumin with phenyhydrazine/ substituted phenyhydrazine derivatives in AcOH. The residue was purified by silica gel column chromatography. Structures of purified compounds were confirmed by 1H NMR and Mass spectroscopy. The synthesized compounds were evaluated for their antibacterial activity by the microdilution broth susceptibility test method against gram positive (S. aureus) and gram negative (E. coli). Results: Effects of substitution in N-phenylpyrazole curcumin derivatives against S. aureus and E. coli were studied. The most active N-(3-Nitrophenylpyrazole) curcumin (12) exhibits twenty-fold more potency against S. aureus (MIC: 10μg/mL)) and N-(2-Fluoroophenylpyrazole) curcumin (5) fivefold more potency against E. coli (MIC; 50 μg/mL) than N-phenylpyrazole curcumin (4). Whereas, a remarkable decline in anti-bacterial activity against S. aureus and E. coli was observed when electron donating groups were incorporated in N-phenylpyrazole curcumin (4). Comparative studies of synthesized compounds suggest the effects of electron withdrawing and electron donating groups on unsubstituted phenylpyrazole curcumin (4). Conclusion: The structure-activity relationship (SAR) results indicated that the electron withdrawing and electron donating at N-phenylpyrazole curcumin played key roles for their bacterial inhibitory effects. The results of the antibacterial evaluation showed that the synthesized pyrazole derivatives of curcumin displayed moderate to very high activity in S. aureus. In conclusion, the series of novel curcumin derivatives were designed, synthesized and tested for their antibacterial activities against S. aureus and E. coli. Among them, N-(3-Nitrophenylpyrazole curcumin; 12) was most active against S. aureus (Gram-positive) and N-(2-Fluoroophenylpyrazole) curcumin (5) against E. coli (Gram-negative) bacteria.

scholarly journals N-Doped Carbon Quantum Dots as Fluorescent Bioimaging Agents

Crystals ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 789
Author(s):  
Shih-Fu Ou ◽  
Ya-Yun Zheng ◽  
Sin-Jen Lee ◽  
Shyi-Tien Chen ◽  
Chien-Hui Wu ◽  
...  
Keyword(s):  
Quantum Dots ◽  
Carbon Nanomaterials ◽  
Graphene Quantum Dots ◽  
Carbon Quantum Dots ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Fluorescence Characteristics ◽  
And Staphylococcus Aureus

Graphene quantum dots, carbon nanomaterials with excellent fluorescence characteristics, are advantageous for use in biological systems owing to their small size, non-toxicity, and biocompatibility. We used the hydrothermal method to prepare functional N-doped carbon quantum dots (N-CQDs) from 1,3,6-trinitropyrene and analyzed their ability to fluorescently stain various bacteria. Our results showed that N-CQDs stain the cell septa and membrane of the Gram-negative bacteria Escherichia coli, Salmonellaenteritidis, and Vibrio parahaemolyticus and the Gram-positive bacteria Bacillus subtilis, Listeria monocytogenes, and Staphylococcus aureus. The optimal concentration of N-CQDs was approximately 500 ppm for Gram-negative bacteria and 1000 ppm for Gram-positive bacteria, and the exposure times varied with bacteria. N-Doped carbon quantum dots have better light stability and higher photobleaching resistance than the commercially available FM4-64. When excited at two different wavelengths, N-CQDs can emit light of both red and green wavelengths, making them ideal for bioimaging. They can also specifically stain Gram-positive and Gram-negative bacterial cell membranes. We developed an inexpensive, relatively easy, and bio-friendly method to synthesize an N-CQD composite. Additionally, they can serve as a universal bacterial membrane-staining dye, with better photobleaching resistance than commercial dyes.

scholarly journals Gram-positive bacteria cell wall-derived lipoteichoic acid induces inflammatory alveolar bone loss through prostaglandin E production in osteoblasts

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Tsukasa Tominari ◽  
Ayumi Sanada ◽  
Ryota Ichimaru ◽  
Chiho Matsumoto ◽  
Michiko Hirata ◽  
...  
Keyword(s):  
Cell Wall ◽  
Bone Loss ◽  
Alveolar Bone ◽  
Osteoclast Differentiation ◽  
Lipoteichoic Acid ◽  
Alveolar Bone Loss ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria

AbstractPeriodontitis is an inflammatory disease associated with severe alveolar bone loss and is dominantly induced by lipopolysaccharide from Gram-negative bacteria; however, the role of Gram-positive bacteria in periodontal bone resorption remains unclear. In this study, we examined the effects of lipoteichoic acid (LTA), a major cell-wall factor of Gram-positive bacteria, on the progression of inflammatory alveolar bone loss in a model of periodontitis. In coculture of mouse primary osteoblasts and bone marrow cells, LTA induced osteoclast differentiation in a dose-dependent manner. LTA enhanced the production of PGE2 accompanying the upregulation of the mRNA expression of mPGES-1, COX-2 and RANKL in osteoblasts. The addition of indomethacin effectively blocked the LTA-induced osteoclast differentiation by suppressing the production of PGE2. Using ex vivo organ cultures of mouse alveolar bone, we found that LTA induced alveolar bone resorption and that this was suppressed by indomethacin. In an experimental model of periodontitis, LTA was locally injected into the mouse lower gingiva, and we clearly detected alveolar bone destruction using 3D-μCT. We herein demonstrate a new concept indicating that Gram-positive bacteria in addition to Gram-negative bacteria are associated with the progression of periodontal bone loss.

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