scholarly journals Silver-calcium-borates as better replacement for conventional organic antimicrobials in cosmetic products

2022 ◽  
Vol 11 (1) ◽  
pp. 113-120 ◽  
Author(s):  
A.L. Arunachalam ◽  
S. Induja ◽  
V. Parthasarathy ◽  
P.S. Raghavan
Keyword(s):  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Xrd Analysis ◽  
New Drugs ◽  
The Novel ◽  
Cosmetic Products ◽  
Bacterial Reduction ◽  
Phase Purity ◽  
Powder Xrd Analysis ◽  
Antibacterial And Antifungal

Microbes generally develop resistance towards organic antibacterial agents like ampicillin, Sulfonamides, methicillin, etc., and progressively new drugs are being invented to replace them. Hence, replacement of organic antibacterial agents with inorganic analogues requires constant research and the present investigation reports alternatives for conventional antimicrobial agents like methylparaben, diazolidinyl urea, etc., in the cosmetic products with silver incorporated calcium borates. The chemically synthesized silver-calcium borates have been analyzed for phase purity using powder XRD analysis, nature of bonding using FTIR vibrations, and morphology using SEM. The antibacterial and antifungal studies were carried out for the novel inorganic silver-calcium borates incorporated cosmetic products. The products were also subjected to thermal & photostability studies and found to be comparable with that of commercially available products. A minimum quantity of 3 ppm of silver-calcium borate concentration was required to bring about nearly 100% bacterial reduction in the cosmetic products.

Synthesis, in silico pharmacokinetics and biological evaluation of some new thiazolidinedione as PPAR-γ agonists and antibacterial agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Zohor Mohammad Mahdi Alzhrani ◽  
Mohammad Mahboob Alam ◽  
Syed Nazreen
Keyword(s):  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Antibacterial Activities ◽  
Biological Evaluation ◽  
New Drugs ◽  
Diabetic Patients ◽  
Spectroscopic Techniques ◽  
Standard Drug ◽  
Ppar Γ

Background: The frequent uses of antimicrobial agents to treat infections in diabetic patients make them more drug resistance than non diabetic patients which accounts for higher mortality rate of diabetic patients. Therefore, it is a necessity today to synthesize new drugs with dual mode of action as antidiabetic and antibacterial agents. In the present work, new derivatives containing thiazolidinedione and 1,3,4-oxadiaozle have been synthesized and screened for PPAR-γ and antibacterial activities. Methods: Compound 5-12 have been synthesized from 2-methoxy benzaldehyde and thiazolidinedione and characterized using different spectroscopic techniques such as IR, NMR and mass spectrometry. These compounds were tested for in vitro PPAR-γ transactivation, PPAR-γ gene expression and antibacterial activities. Finally molecular docking was carried out to see the binding interactions of molecules with the target protein. Results: All the compounds follow Lipinski rule suggesting the synthesized derivatives have good drug likeness properties. Compound 11 and 12 exhibited promising PPAR-γ transactivation with 73.69% and 76.50%, respectively as well as showed significant antibacterial activity with comparable MIC of 3.12 μg/disc to standard drug amoxicillin. The docking result was found to be in consistent with the in vitro PPAR-γ transactivation results. Conclusion: Compounds 11 and 12 can be further investigated as lead molecules for the development of new and effective antidiabetic and antibacterial agents.

scholarly journals UHPLC-ESI-QTOF-MS/MS-Based Molecular Networking Guided Isolation and Dereplication of Antibacterial and Antifungal Constituents of Ventilago denticulata

Antibiotics ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 606 ◽  
Author(s):  
Muhaiminatul Azizah ◽  
Patcharee Pripdeevech ◽  
Tawatchai Thongkongkaew ◽  
Chulabhorn Mahidol ◽  
Somsak Ruchirawat ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Herbal Medicine ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Antifungal Agents ◽  
Flavonoid Glycosides ◽  
Antimicrobial Compounds ◽  
Molecular Networking ◽  
Fragment Ions ◽  
Antibacterial And Antifungal

Ventilago denticulata is an herbal medicine for the treatment of wound infection; therefore this plant may rich in antibacterial agents. UHPLC-ESI-QTOF-MS/MS-Based molecular networking guided isolation and dereplication led to the identification of antibacterial and antifungal agents in V. denticulata. Nine antimicrobial agents in V. denticulata were isolated and characterized; they are divided into four groups including (I) flavonoid glycosides, rhamnazin 3-rhamninoside (7), catharticin or rhamnocitrin 3-rhamninoside (8), xanthorhamnin B or rhamnetin 3-rhamninoside (9), kaempferol 3-rhamninoside (10) and flavovilloside or quercetin 3-rhamninoside (11), (II) benzisochromanquinone, ventilatones B (12) and A (15), (III) a naphthopyrone ventilatone C (16) and (IV) a triterpene lupeol (13). Among the isolated compounds, ventilatone C (16) was a new compound. Moreover, kaempferol, chrysoeriol, isopimpinellin, rhamnetin, luteolin, emodin, rhamnocitrin, ventilagodenin A, rhamnazin and mukurozidiol, were tentatively identified as antimicrobial compounds in extracts of V. denticulata by a dereplication method. MS fragmentation of rhamnose-containing compounds gave an oxonium ion, C6H9O3+ at m/z 129, while that of galactose-containing glycosides provided the fragment ion at m/z 163 of C6H11O5+. These fragment ions may be used to confirm the presence of rhamnose or galactose in mass spectrometry-based analysis of natural glycosides or oligosaccharide attached to biomolecules, that is, glycoproteins.

scholarly journals Antibacterial, antifungal, and antiviral activities of chalcone-bearing tetrahydropyranyl and 2,4-dihydroxyl moieties

2020 ◽  
Vol 49 (1) ◽  
Author(s):  
William Gustavo Lima ◽  
Jéssica Tauany Andrade ◽  
Felipe Rocha da Silva Santos ◽  
Juliana Maria Campos Palumbo ◽  
Karina Marjorie Silva Herrera ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
New Drugs ◽  
Bacteriostatic Effect ◽  
Virus Serotype ◽  
Antifungal Effects ◽  
Antiviral Activities ◽  
Resistant Strains ◽  
Antibacterial And Antifungal ◽  
Dengue Virus Serotype 2 ◽  
Important Structure

Chalcones highlights as an important structure in medicinal chemistry and thus has been widely used as a template in the development of new drugs. In this study, we aim to determine the antibacterial, anti-Candida, and anti-Dengue potential of new chalcone-bearing 2,4-dihydroxyl and tetrahydropyranyl moieties. Antimicrobial activity assays showed that microorganism of the Staphylococcus genus (including methicillin-resistant strains) were susceptible to 2,4-dihydroxychalcones, with minimum inhibitory concentrations (MICs) ranging of 19.5 to 125 µg.mL-1. Compound 4e, which showed the highest bacteriostatic effect, also has bactericidal activity from of 80 µg.mL-1. The growth of oral isolates of Candida albicans was also efficiently inhibited with compound 4e (MIC: 15.6–32.3 µg.mL-1), which was fungicidal at 15.6 µg.mL-1. However, the presence of the tetrahydropyranyl moiety impaired both the antibacterial and antifungal effects. None of the chalcones tested were actives against Dengue virus serotype 2. In conclusion, the compound 4e showed good anti-Staphylococci and anti-Candida activity and may be a promising prototype for the development of new antimicrobial agents.

scholarly journals 1,2,4-Triazoles as Important Antibacterial Agents

2021 ◽  
Vol 14 (3) ◽  
pp. 224
Author(s):  
Małgorzata Strzelecka ◽  
Piotr Świątek
Keyword(s):  
Drug Resistance ◽  
Antibacterial Activity ◽  
Biological Activity ◽  
Rational Design ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Triazole Ring ◽  
The Novel ◽  
Global Spread ◽  
Antibacterial Potential

The global spread of drug resistance in bacteria requires new potent and safe antimicrobial agents. Compounds containing the 1,2,4-triazole ring in their structure are characterised by multidirectional biological activity. A large volume of research on triazole and their derivatives has been carried out, proving significant antibacterial activity of this heterocyclic core. This review is useful for further investigations on this scaffold to harness its optimum antibacterial potential. Moreover, rational design and development of the novel antibacterial agents incorporating 1,2,4-triazole can help in dealing with the escalating problems of microbial resistance.

scholarly journals Synthesis, antibacterial and antifungal activity of 1-[4-(1,1,3,3-tetramethylbutyl)phenoxy]-3-dialkylamino-2-propanol quaternary salts

2019 ◽  
pp. 56-62 ◽  
Author(s):  
Y. V. Korotkii ◽  
N. A. Vrynchanu ◽  
M. L. Dronova ◽  
Z. S. Suvorova ◽  
O. A. Smertenko
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Dilution Method ◽  
The Novel ◽  
Antibacterial And Antifungal Activity ◽  
Antimicrobial Drugs ◽  
Quaternary Salts ◽  
Resistant Strains ◽  
Antibacterial And Antifungal

The emergence and spread of resistant strains of pathogens as well as reduction of the efficacy of current antimicrobial agents requires the development of novel antimicrobial compounds. The aim of the present study was synthesis and evaluation of antimicrobial activity of new arylaliphatic aminopropanols. The objects of the present study were 1-[4-(1,1,3,3-tetramethylbutyl)phenoxy]-3-dialkylamino-2-propanol quaternary salts (compounds I–XIV). Compounds synthesis was carried out by heating of precursor epoxide and excessive amount of appropriate amines in isopropanole, followed by treatment with excess of alkyl halides. Methods of elemental analysis, IR- and PMR-spectroscopy were used for confirmation of chemical structure. Antimicrobial activity against Staphylococcus аureus АTCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa АТСС 27853 and Candida albicans NCTC 885/653 was determined by a broth dilution method and evaluated via minimum inhibitory concentration (MIC). Our investigation of antibacterial and antifungal activity of 1-[4-(1,1,3,3-tetra methylbutyl)phenoxy]-3-dialkylamino-2-propanol quaternary salts showed that compounds possess narrow spectrum, as well as broad spectrum action. Significant antimicrobial activity of the novel aryl aliphatic aminoalcohols indicates their potential usage as a component of new antimicrobial drugs.

Antimicrobial agents

2017 ◽  
Author(s):  
Katherine E. Walton ◽  
Sally Ager
Keyword(s):  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Antifungal Agents ◽  
Clinical Status ◽  
Antimicrobial Treatment ◽  
Routes Of Administration ◽  
Inappropriate Use ◽  
Antibacterial And Antifungal ◽  
Special Factors ◽  
Practice Patient

Antimicrobial resistance is a growing problem, which can be exacerbated by inappropriate use of antimicrobial agents. An understanding of the judicious use of antimicrobial agents, also known as antimicrobial stewardship, is therefore of fundamental importance to safe clinical practice. Patient factors should also be considered, including age, clinical status, special factors such as pregnancy or immunosuppression, co-morbidities, allergies, medication which may result in potential drug interactions, previous microbiology results, and antimicrobial treatment history. Important antimicrobial characteristics include the drug’s spectrum of activity, routes of administration, potential side effects, and cost. This chapter provides an overview of the ways in which antibacterial agents work and how bacteria develop resistance. It also outlines the principles of safe antimicrobial prescribing for prophylaxis and therapy, and highlights the key features, clinical indications, and potential adverse effects of antibacterial and antifungal agents commonly used in urology.

scholarly journals Reusable Nano-Zirconia-Catalyzed Synthesis of Benzimidazoles and Their Antibacterial and Antifungal Activities

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4219
Author(s):  
Tentu Nageswara Rao ◽  
Suliman Yousef AlOmar ◽  
Faheem Ahmed ◽  
Fadwa Albalawi ◽  
Naushad Ahmad ◽  
...  
Keyword(s):  
Bond Formation ◽  
Xrd Analysis ◽  
One Pot ◽  
Hydrothermal Technique ◽  
Phase Purity ◽  
Antibacterial And Antifungal Activities ◽  
Fused Heterocycles ◽  
Nano Catalyst ◽  
Antibacterial And Antifungal ◽  
Synthesized Materials

In this article, a zirconia-based nano-catalyst (Nano-ZrO2), with intermolecular C-N bond formation for the synthesis of various benzimidazole-fused heterocycles in a concise method is reported. The robustness of this reaction is demonstrated by the synthesis of a series of benzimidazole drugs in a one-pot method. All synthesized materials were characterized using 1HNMR, 13CNMR, and LC-MS spectroscopy as well as microanalysis data. Furthermore, the synthesis of nano-ZrO2 was processed using a standard hydrothermal technique in pure form. The crystal structure of nano-ZrO2 and phase purity were studied, and the crystallite size was calculated from XRD analysis using the Debye–Scherrer equation. Furthermore, the antimicrobial activity of the synthesized benzimidazole drugs was evaluated in terms of Gram-positive, Gram-negative, and antifungal activity, and the results were satisfactory.

Discovery of Antibacterial Agents Inhibiting the Energy-Coupling Factor (ECF) Transporters by Structure-Based Virtual Screening

2020 ◽  
Author(s):  
Eleonora Diamanti ◽  
Inda Setyawati ◽  
Spyridon Bousis ◽  
leticia mojas ◽  
lotteke Swier ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Energy Coupling ◽  
Coupling Factor ◽  
Design Synthesis ◽  
Screening Design ◽  
Starting Point ◽  
Wide Range ◽  
Vitamin Uptake

Here, we report on the virtual screening, design, synthesis and structure–activity relationships (SARs) of the first class of selective, antibacterial agents against the energy-coupling factor (ECF) transporters. The ECF transporters are a family of transmembrane proteins involved in the uptake of vitamins in a wide range of bacteria. Inhibition of the activity of these proteins could reduce the viability of pathogens that depend on vitamin uptake. Because of their central role in the metabolism of bacteria and their absence in humans, ECF transporters are novel potential antimicrobial targets to tackle infection. The hit compound’s metabolic and plasma stability, the potency (20, MIC Streptococcus pneumoniae = 2 µg/mL), the absence of cytotoxicity and a lack of resistance development under the conditions tested here suggest that this scaffold may represent a promising starting point for the development of novel antimicrobial agents with an unprecedented mechanism of action.<br>

Novel Thiazole-Based Thiazolidinones as Potent Anti-infective Agents: In silico PASS and Toxicity Prediction, Synthesis, Biological Evaluation and Molecular Modelling

2020 ◽  
Vol 23 (2) ◽  
pp. 126-140 ◽  
Author(s):  
Christophe Tratrat
Keyword(s):  
In Silico ◽  
Antimicrobial Agents ◽  
Target Identification ◽  
Biological Evaluation ◽  
Microbial Infection ◽  
Toxicity Prediction ◽  
Discovery Studio ◽  
Bacteria And Fungi ◽  
Multiple Drugs ◽  
Antibacterial And Antifungal

Aims and Objective: The infectious disease treatment remains a challenging concern owing to the increasing number of pathogenic microorganisms associated with resistance to multiple drugs. A promising approach for combating microbial infection is to combine two or more known bioactive heterocyclic pharmacophores in one molecular platform. Herein, the synthesis and biological evaluation of novel thiazole-thiazolidinone hybrids as potential antimicrobial agents were dissimilated. Materials and Methods: The preparation of the substituted 5-benzylidene-2-thiazolyimino-4- thiazolidinones was achieved in three steps from 2-amino-5-methylthiazoline. All the compounds have been screened in PASS antibacterial activity prediction and in a panel of bacteria and fungi strains. Minimum inhibitory concentration and minimum bacterial concentration were both determined by microdilution assays. Molecular modeling was conducted using Accelrys Discovery Studio 4.0 client. ToxPredict (OPEN TOX) and ProTox were used to estimate the toxicity of the title compounds. Results: PASS prediction revealed the potentiality antibacterial property of the designed thiazolethiazolidinone hybrids. All tested compounds were found to kill and to inhibit the growth of a vast variety of bacteria and fungi, and were more potent than the commercial drugs, streptomycin, ampicillin, bifomazole and ketoconazole. Further, in silico study was carried out for prospective molecular target identification and revealed favorable interaction with the target enzymes E. coli MurB and CYP51B of Aspergillus fumigatus. Toxicity prediction revealed that none of the active compounds was found toxic. Conclusion: Substituted 5-benzylidene-2-thiazolyimino-4-thiazolidinones, endowing remarkable antibacterial and antifungal properties, were identified as a novel class of antimicrobial agents and may find a potential therapeutic use to eradicate infectious diseases.

Copper-catalyzed Convenient Synthesis and SAR Studies of Substituted-1,2,3-triazole as Antimicrobial Agents

2018 ◽  
Vol 16 (1) ◽  
pp. 3-10
Author(s):  
Aniket P. Sarkate ◽  
Kshipra S. Karnik ◽  
Pravin S. Wakte ◽  
Ajinkya P. Sarkate ◽  
Ashwini V. Izankar ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
One Pot ◽  
Triazole Derivatives ◽  
Sar Studies ◽  
Convenient Synthesis ◽  
Antibacterial And Antifungal

Background:A novel copper-catalyzed synthesis of substituted-1,2,3-triazole derivatives has been developed and performed by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The reaction is one-pot multicomponent.Objective:We state the advancement and execution of a methodology allowing for the synthesis of some new substituted 1,2,3-triazole analogues with antimicrobial activity.Methods:A series of triazole derivatives was synthesized by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, IR, MS and elemental analysis. All the synthesized compounds were tested for their antimicrobial activity against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus nigar for antifungal activity, respectively.Results and Conclusion:From the antimicrobial data, it was observed that all the newly synthesized compounds showed good to moderate level of antibacterial and antifungal activity.

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