Antimicrobial Potential of Nicotinic Acid Derivatives Against Various Pathogenic Microbes

Asif, Mohammad

doi:10.13187/ercr.2014.1.10

Cited by 10 publications

(5 citation statements)

References 23 publications

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“…Nicotinic acid has ability to show anti-bacterial activity as reported in the literature. [38][39][40][41] So, we extend our study and make a functionalized series of compounds (5a-5h) from 2-bromoisonicotinate (3) using SMC.…”

Section: Discussionmentioning

confidence: 84%

Synthesis, Anti-Bacterial and Molecular Docking Studies of Arylated Butyl 2-Bromoisonicotinate Against Clinical Isolates of ESBL-Producing Escherichia coli ST405 and Methicillin-Resistant Staphylococcus aureus

Naheed,

Din,

Qamar

et al. 2023

IDR

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Introduction: Global public health concerns include the emergence and spread of methicillin-resistant Staphylococcus aureus (MRSA) and extended-spectrum beta-lactamase Escherichia coli (ESBL-E. coli). These pathogens cause infections that are difficult to treat, which can have fatal outcomes and require lengthy hospital stays. As a result, we created butyl 2-bromoisonicotinate and tested its antibacterial effectiveness against the ESBL-E. coli ST 405 and MRSA pathogens. Natural product discovery is complemented by synthetic compound synthesis because of the latter's potential for superior characteristics, target specificity, scalability, intellectual advantages, and chemical diversity. Because of this, the potential for discovering new medicinal compounds is increased, and the constraints placed on natural sources are overcome. Natural items are tough to obtain since they are hard to isolate and synthesize. Therefore, modern science is actively searching for small molecules as therapeutic agents by applying sustainable techniques that can be commercialized. Methods: Two patients' blood samples were taken, and the BACTEC/Alert system was used to process them. On blood and MacConkey agar, the positive samples were subcultured and incubated aerobically at 37 °C. Using the VITEK 2 compact system, the isolates were subjected to isolate identification and MIC. MLST of the ESBL-E. coli was performed by PCR. Additionally, Fischer esterification was used to create butyl 2-bromoisonicotinate in excellent yields. A commercially available palladium catalyst was then used to arylate the compound, resulting in medium to good yields of arylated butyl 2-bromoisonicotinates. Using the agar well diffusion assay and the micro-broth dilution method, we assessed the in-vitro activities of the synthesized molecules (3, 5a-h) against clinically isolated ESBL-E. coli ST405, and MRSA. A molecular operating environment was used to carry out in silico validation of the synthesized compounds' binding to the active site and to evaluate the stability of their molecular interactions with the target E. coli 2Y2T protein.Results: MRSA and ESBL-producing E. coli were identified as the two clinical isolates. While MRSA was also resistant to betalactam drugs and least resistant to vancomycin, ESBL-producing E. coli belonged to ST405 and was resistant to cephalosporins and sensitive to carbapenems. Good yields of the desired compounds were produced by our effective and economical synthesis. By using a micro-broth dilution assay, the Molecules (3, 5a, and 5d) were most effective against both resistant strains. The Molecules (3, 5a, 5b, and 5d) also displayed good binding energies. Conclusion:The butyl 2-bromoisonicotinate displayed antibacterial efficacy against ESBL-producing E. coli ST405 and MRSA strains. After the in-vivo trial, this substance might offer an alternative therapeutic option.

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Section: Discussionmentioning

confidence: 84%

Synthesis, Anti-Bacterial and Molecular Docking Studies of Arylated Butyl 2-Bromoisonicotinate Against Clinical Isolates of ESBL-Producing Escherichia coli ST405 and Methicillin-Resistant Staphylococcus aureus

Naheed,

Din,

Qamar

et al. 2023

IDR

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“…Several authors have confirmed "neem" and its compounds as a powerful and promising antifungal agent against medically important dermatophytes from the genera Microsporum , Trichophyton, and Epidermophyton that commonly cause skin disease [ 14 , 15 ]. Baby et al [ 16 ] compiled a collection of recent studies and patents that address the effectiveness of neem in treating acne and other common skin disorders.…”

Section: Discussionmentioning

confidence: 99%

Antifungal Activity of Neem Leaf Extract With Eucalyptus citriodora Oil and Cymbopogon martini Oil Against Tinea Capitis: An In-Vitro Evaluation

Tiple,

Jamane,

Khobragade

2024

Cureus

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IntroductionTinea capitis, often known as ringworm of the scalp, is a fungal infection that affects the scalp, eyelashes, and eyebrows. It is generally caused by dermatophytes from the genera Trichophyton and Microsporum. Trichophyton tonsurans and Microsporum canis are the main etiological agents responsible for most of the cases of tinea capitis globally. Tinea capitis commonly manifests as itchy, scaly patches of hair loss. Tinea capitis is the prevailing dermatophyte illness among children globally. MethodsAn in-vitro evaluation study was conducted to assess the antifungal properties of ethanolic extracts of neem leaves and the oils of Eucalyptus citriodora and Cymbopogon martini, both individually and in combination. The agar-well diffusion method and the M38-A2 microbroth dilution method were employed to evaluate the antifungal efficacy against pathogenic dermatophyte strains, namely Microsporum canis and Trichophyton tonsurans. The fully mature green leaves were treated with ethanol to make the neem leaf extract. Additionally, high-performance liquid chromatographic analysis was carried out to determine the contents of the terpenoids. Fluconazole, an antifungal drug, is used as a standard. ResultsThe findings demonstrated an overall inhibition of the growth of dermatophytes at a minimal inhibitory concentration of 187.5 and 375 μg/ml for neem leaf extract and 0.625 to 2.5 μl/ml for selected herbal oils, whereas it was 0.25 μg/ml and 0.50 μg/ml for positive control against Microsporum canis and Trichophyton tonsurans, respectively. ConclusionThe phytochemical investigation of the ethanolic extracts in neem leaves revealed the presence of terpenoids, which are known for their significant biological activity. The study's findings demonstrated the therapeutic capabilities of neem leaf extract in combination with the oils of Eucalyptus citriodora and Cymbopogon martini for managing the tinea capitis infection. A broader and improved antifungal spectrum was seen when neem leaf extract and oils were combined. Therefore, it can be developed into a suitable formulation for the management of tinea capitis.

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“…Dietary sources rich in nicotinic acid include meat, fish, nuts, and whole grains. Antibacterial activity of nicotinic acid has been reported (Bartzatt et al 2007;Asif 2014;Osigbemhe et al 2022). However, the efficacy of nicotinic acid on S. pneumoniae biofilm remains not well investigated.…”

Section: Introductionmentioning

confidence: 99%

Inhibitory Effects of Nicotinic Acid against <em>Streptococcus pneumoniae </em>Biofilm

Rosdi,

Bahri

2024

Preprint

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This study was performed to evaluate the efficacy of nicotinic acid against Streptococcus pneumoniae biofilm. The experimental results indicate that S. pneumoniae forms biofilms, particularly at the liquid-air interface, as evidenced by the pellicle assay. Nicotinic acid demonstrated significant inhibition of S. pneumoniae biofilm formation at 6 h and 18 h, with higher concentrations leading to lower biofilm biomass, suggesting a concentration-dependent response. However, minimal biofilm inhibition was observed at 12 h. Treatment with nicotinic acid induced FTIR spectral changes in protein biomolecules of S. pneumoniae biofilm at 6 h and 18 h, evidenced by alterations in spectral peaks at 750 cm-1, 906 cm-1, 1540 cm-1, 1548 cm-1, and 1644 cm-1. Notably, no FTIR spectral changes were detected in 12 h S. pneumoniae biofilm following exposure to nicotinic acid. These findings suggest that nicotinic acid inhibits biofilm formation in a time and concentration-dependent manner, possibly by altering the structure of protein biomolecules within the biofilm.

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Antimicrobial Potential of Nicotinic Acid Derivatives Against Various Pathogenic Microbes

Cited by 10 publications

References 23 publications

Synthesis, Anti-Bacterial and Molecular Docking Studies of Arylated Butyl 2-Bromoisonicotinate Against Clinical Isolates of ESBL-Producing Escherichia coli ST405 and Methicillin-Resistant Staphylococcus aureus

Synthesis, Anti-Bacterial and Molecular Docking Studies of Arylated Butyl 2-Bromoisonicotinate Against Clinical Isolates of ESBL-Producing Escherichia coli ST405 and Methicillin-Resistant Staphylococcus aureus

Antifungal Activity of Neem Leaf Extract With Eucalyptus citriodora Oil and Cymbopogon martini Oil Against Tinea Capitis: An In-Vitro Evaluation

Inhibitory Effects of Nicotinic Acid against <em>Streptococcus pneumoniae </em>Biofilm

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