scholarly journals Design, Synthesis and Biological Assessment of Thiazole Derivatives as Possible Antioxidant and Antimicrobial Agents

2021 ◽  
pp. 24-32
Author(s):  
. Isha ◽  
Neetu Sachan
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Therapeutic Potential ◽  
Antibacterial Properties ◽  
Antimicrobial Properties ◽  
Molecular Structures ◽  
Biological Assessment ◽  
Thiazole Derivatives ◽  
Antioxidant And Antimicrobial Activity

Aims: To synthesize thiazole derivatives and evaluate their therapeutic potential to continue our quest for new antibacterial and antioxidant drugs. Place and Duration of Study: Institute of Pharmaceutical Research, GLA University, Mathura, Uttar Pradesh, between January 2021 and July 2021. Methodology: The target compounds in this investigation were synthesized in the search for new molecules having antioxidant and antimicrobial activity. Physicochemical and spectroanalytical studies validated the derivatives molecular structures. Antioxidant and antimicrobial properties of the synthesized molecules were evaluated in vitro using the DPPH and tube dilution methods, respectively. Results: The majority of the synthesized derivatives displayed antioxidant and antimicrobial activity. The efficacy of the derivatives varied based upon the substituent. Compound 7c exhibited significant antioxidant and antibacterial activity, according to the results of the study. Conclusion: Our results showed the antioxidant and antibacterial properties of novel thiazole compounds, implying the probability of their utilization in the development of new therapeutics.

scholarly journals An In Vitro Study on the Antimicrobial Properties of Essential Oil Modified Resin Composite against Oral Pathogens

Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Resin Composite ◽  
Antimicrobial Properties ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Oral Pathogens

Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.

scholarly journals Evaluating the Antimicrobial Activity of Commercially Available Herbal Toothpastes on Microorganisms Associated with Diabetes Mellitus

2013 ◽  
Vol 14 (5) ◽  
pp. 924-929 ◽  
Author(s):  
Reena Kulshrestha ◽  
J Kranthi ◽  
P Krishna Rao ◽  
Feroz Jenner ◽  
V Abdul Jaleel ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Antimicrobial Activity ◽  
Dental Health ◽  
Antibacterial Properties ◽  
Antimicrobial Properties ◽  
Test Organism ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Disk Diffusion Method

ABSTRACT Aim The present study was conducted to evaluate the efficacy of commercially available herbal toothpastes against the different periodontopathogens. Materials and methods Six herbal toothpastes that were commonly commercially available were included in the study. Colgate herbal, Babool, Meswak, Neem active, Dabur red toothpastes were tested for the study whereas sterile normal saline was used as control. Antimicrobial efficacies of dentifrices were evaluated against Streptococcus mutans and Actinobacillus actinomycetemcomitans. The antimicrobial properties of dentifrices were tested by measuring the maximum zone of inhibition at 24 hours on the Mueller Hinton Agar media inoculated with microbial strain using disk diffusion method. Each dentifrice was tested at 100% concentration (full strength). Results The study showed that all dentifrices selected for the study were effective against the entire test organism but to varying degree. Neem active tooth paste gave a reading of 25.4 mm as the zone of inhibition which was highest amongst all of the test dentifrices. Colgate Herbal and Meswak dentifrices recorded a larger maximum zone of inhibition, measuring 23 and 22.6 mm respectively, compared to other toothpastes. All other dentifrices showed the zone of inhibition to be between 17 and 19 mm respectively. Conclusion The antibacterial properties of six dentifrices were studied in vitro and concluded that almost all of the dentifrices available commercially had antibacterial properties to some extent to benefit dental health or antiplaque action. How to cite this article Jenner F, Jaleel VA, Kulshrestha R, Maheswar G, Rao PK, Kranthi J. Evaluating the Antimicrobial Activity of Commercially Available Herbal Toothpastes on Microorganisms Associated with Diabetes Mellitus. J Contemp Dent Pract 2013;14(5):924-929.

scholarly journals Antimicrobial Activity from Species Plectranthus amboinicus (Lour.) Spreng, a Review

2020 ◽  
pp. 1-14
Author(s):  
Juliane Maria dos Santos Silva ◽  
Jackson Roberto Guedes da Silva Almeida ◽  
Cristiane dos Santos Cerqueira Alves ◽  
Daniel Amando Nery ◽  
Livia Maria Oliveira Damasceno ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Therapeutic Potential ◽  
In Vivo Studies ◽  
Synergistic Activity ◽  
Popular Medicine ◽  
Plectranthus Amboinicus

Introduction: Nowadays, several bacteria have acquired resistance to available antimicrobial agents making necessary the search for new therapeutic alternatives. Plectranthus amboinicus L. is a succulent and aromatic herb, popularly known as thick leaf mint, used in popular medicine for the treatment of colds, digestive diseases, asthma, headache and to fight pathogenic bacteria activity. In view the antimicrobial activity of P. amboinicus this study had as aim to review publications involving researches about antimicrobial activity of this species. Materials and Methods: For this, PubMed, Scopus, Science Direct and Scielo databases were consulted in November 2020 using the keywords Plectranthus amboinicus and antimicrobial activity. In vitro and/or in vivo studies on the antimicrobial activity of the species in the last 10 years were considered. Results: The main microorganisms evaluated were: Klebsiella pneumoniae, Mycobacterium tuberculosis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and some Candida species. The essential oils had carvacrol, germacrene D, thymol and camphor as main constituents. Most studies evaluated the antimicrobial activity using broth dilution and agar diffusion methods. In most studies essential oil, extracts and/or isolated substances showed significant antimicrobial activity. Synergistic activity was also observed through association with antibiotics. Conclusion: P. amboinicus has therapeutic potential for antimicrobial treatments and can be an alternative to the treatment of resistant microorganisms and that further in vivo and clinical studies with the species are still needed.

New Caffeic Acid Derivatives as Antimicrobial Agents: Design, Synthesis, Evaluation and Docking

2019 ◽  
Vol 19 (4) ◽  
pp. 292-304 ◽  
Author(s):  
Maia Merlani ◽  
Vakhtang Barbakadze ◽  
Lela Amiranashvili ◽  
Lali Gogilashvili ◽  
Vladimir Poroikov ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Caffeic Acid ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antimicrobial Properties ◽  
Synthesis Methods ◽  
Design Synthesis ◽  
Caffeic Acid Derivatives ◽  
Microdilution Method

Background: Phenolic acids (caffeic-, ferulic and p-coumaric acid) are widely distributed in the plant kingdom and exhibit broad spectrum of biological activities, including antimicrobial activity. Objective: The goal of this paper is the synthesis of some caffeic acid derivatives selected based on computer-aided predictions and evaluate their in vitro antimicrobial properties against Gram positive and Gram negative bacteria and also a series of fungi. Methods: In silico prediction of biological activity was used to identify the most promising structures for synthesis and biological testing, and the putative mechanisms of their antimicrobial action. The designed compounds were synthesized using classical organic synthesis methods. The antimicrobial activity was studied using microdilution method. Results: Twelve tested compounds have shown good antibacterial activity. Five out of twelve tested compounds appeared to be more active than the reference drugs ampicillin and streptomycin. Despite that all compounds exhibited good activity against all bacteria tested, the sensitivity of bacteria towards compounds in general was different. The evaluation of antifungal activity revealed that all compounds were more active than ketoconazole, while seven compounds (2, 3, 4, 5, 7, 8 and 12) appeared to be more active than bifonazole. Docking results indicate that gyrase inhibition is the putative mechanism of antibacterial action while the inhibition of 14α-demethylase may be responsible for antifungal action. Prediction of cytotoxicity by PROTOX showed that compounds are not toxic (LD50 1000-2000 mg/kg). Conclusion: Thirteen compounds, from which six are new ones, were synthesized, and twelve compounds were tested for antimicrobial activity. The studied compounds appeared to be promising potent and non-toxic antimicrobials, which could be considered as leads for new pharmaceutical agents.

scholarly journals DESIGN, SYNTHESIS, AND PHARMACOLOGICAL EVALUATION OF SOME NOVEL BIS-THIAZOLE DERIVATIVES

2018 ◽  
Vol 11 (4) ◽  
pp. 164 ◽  
Author(s):  
Ramesh M Borde ◽  
Satish B Jadhav ◽  
Rahul R Dhavse ◽  
Achut S Munde
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Properties ◽  
Hantzsch Reaction ◽  
Thiazole Derivatives ◽  
Design Synthesis ◽  
Structure Activity ◽  
Elemental Analyses ◽  
And Staphylococcus Aureus ◽  
Toxic Molecule

 Objective: A series of substituted 5,2-bis-thiazoles derivatives were synthesized by Hantzsch reaction and evaluated in vitro for antimicrobial activity against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus. Methods: 2-(4-(benzyloxy)phenyl)-4-methylthiazole-5-carbothioamide were synthesized and allowed to react with various α-haloketones to give 5,2-bis-thiazoles, i.e., 2-(4-(benzyloxy)phenyl)-4-methyl-5-(4-substituted thiazol-2-yl)thiazole derivatives in excellent yield. The synthesized compounds were characterized by spectroscopic methods as well as elemental analyses. They were screened for their antimicrobial activity using the agar diffusion method.Result: Literature survey reveals that the synthesis of 2-(4-(benzyloxy)phenyl)-4-methyl-5-(4-substituted thiazol-2-yl)thiazole, i.e., (5,2-Bis-thiazoles) derivatives (10a-e) was not reported. The entire compound exhibited mild to moderate antimicrobial activity.Conclusion: The antimicrobial results revealed that the synthesized derivatives have significant antimicrobial properties, and further, structure– activity relationship studies may develop more potent and less toxic molecule.

scholarly journals Antimicrobial activity of a novel Spanish propolis against planktonic and sessile oral Streptococcus spp

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
M. Luisa Navarro-Pérez ◽  
Virginia Vadillo-Rodríguez ◽  
Irene Fernández-Babiano ◽  
Ciro Pérez-Giraldo ◽  
M. Coronada Fernández-Calderón
Keyword(s):  
Antimicrobial Activity ◽  
Biofilm Formation ◽  
Bacterial Resistance ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Ethanolic Extract ◽  
Oral Streptococcus ◽  
Ancient Times ◽  
Ethanolic Extract Of Propolis

AbstractIncreased bacterial resistance to traditional antimicrobial agents has prompted the use of natural products with antimicrobial properties such as propolis, extensively employed since ancient times. However, the chemical composition of propolis extracts is extremely complex and has been shown to vary depending on the region and season of collection, due to variations in the flora from which the pharmacological substances are obtained, being therefore essential for their antimicrobial activity to be checked before use. For this purpose, we evaluate the in vitro antimicrobial and anti-biofilm activity of a new and promising Spanish ethanolic extract of propolis (SEEP) on Streptococcus mutans and Streptococcus sanguinis, responsible, as dominant ‘pioneer’ species, for dental plaque. Results reveal that S. sanguinis is more sensitive to SEEP, slowing and retarding its growth considerably with lower concentrations than those needed to produce the same effect in S. mutans. SEEP presents concentration- and time-dependent killing activity and, furthermore, some of the subinhibitory concentrations employed increased biofilm formation even when bacterial growth decreased. Mono and dual-species biofilms were also inhibited by SEEP. Findings obtained clearly show the relevance of using biofilm and subinhibitory concentration models to determine optimal treatment concentrations.

scholarly journals Synthesis, characterization, synergistic antimicrobial properties and molecular docking of sugar modified uridine derivatives

2021 ◽  
Vol 32 (1) ◽  
pp. 6-21
Author(s):  
Jannatul Maowa ◽  
Asraful Alam ◽  
Kazi M. Rana ◽  
Sujan Dey ◽  
Anowar Hosen ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Molecular Docking ◽  
Density Functional ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Docking Study ◽  
Bacterial Strains ◽  
Molecular Docking Study ◽  
Antibacterial And Antifungal Activities

Abstract Nucleosides and their analogues are an important, well-established class of clinically useful medicinal agents that exhibit antiviral and anticancer activity. Thus, our research group has focused on the synthesis of new nucleoside derivatives that could be tested for their broad-spectrum biological activity. In this study, two new series of nucleoside derivatives were synthesized from uridine (1) through facile two-step reactions using the direct acylation method, affording 5’-O-acyl uridine derivatives in good yields. The isolated uridine analogs were further transformed into two series of 2’,3’-di-O-acyl derivatives bearing a wide variety of functionalities in a single molecular framework to evaluate their antimicrobial activity. The new synthesized compounds were characterized through physicochemical, elemental and spectroscopic analysis, and all were screened for their in vitro antimicrobial activity against selected human and plant pathogenic strains. The test compounds revealed moderate to good antibacterial and antifungal activities and were more effective against fungal phytopathogens than against bacterial strains, while many of them exhibited better antimicrobial activity than standard antibiotics. Minimum inhibition concentration (MIC) and minimum bactericidal concentration (MBC) tests against all microorganisms were also conducted for five compounds based on their activity (6, 11, 13, 16, and 17). In addition, all the derivatives were optimized using density functional theory (DFT) B3LYP/6-31g+(d,p) calculations to elucidate their thermal and molecular orbital properties. A molecular docking study was performed using the human protein 5WS1 to predict their binding affinity and modes, and ADMET and SwissADME calculations confirmed the improved pharmacokinetic properties of the compounds. Besides, structure–activity relationship (SAR), thermogravimetric analysis (TGA), and X-ray diffraction (XRD) studies were also performed. Thus, the improvement of the bioactivity of these compounds is expected to significantly contribute to the design of more antimicrobial agents for therapeutic use in the future.

scholarly journals Red Algae as Source of Nutrients with Antioxidant and Antimicrobial Potential

Proceedings ◽  
2020 ◽  
Vol 70 (1) ◽  
pp. 5
Author(s):  
María. Carpena ◽  
Cristina Caleja ◽  
Paula García-Oliveira ◽  
Carla Pereira ◽  
Marina Sokovic ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Organic Acids ◽  
Red Algae ◽  
Antimicrobial Agents ◽  
Biological Properties ◽  
Nutritional Composition ◽  
In Vitro Assays ◽  
Antimicrobial Potential ◽  
Antioxidant And Antimicrobial Activity

Seaweeds have been consumed since ancient times in different cultures, especially in Asian regions. Currently, several scientific studies have highlighted the nutritional value of algae as well as their biological properties. The present work was directed towards the determination of the nutritional composition (ash, protein, fat, carbohydrate content and energy value), the organic acids content, and also the antioxidant and antimicrobial activity of three typical red algae from Galicia: Chondrus crispus, Mastocarpus stellatus and Gigartina pistillata. The nutritional profile was determined by the methods described by AOAC, while organic acids were determined by UPFLC-PDA. The antioxidant activity was assessed using two in vitro assays: TBARS and OxHLIA. At last, antimicrobial activity was tested against two Gram (−), three Gram (+) and three fungus species. The results showed a similar nutritional composition among the three algae, with a low-fat content and a high content of proteins, carbohydrates and energy. Finally, in vitro assays showed significant antioxidant capacity of the three algae and antimicrobial potential against all the tested microorganisms. Thus, the study shows the potential of red algae to be part of the human diet, due to their nutritional content and bioactive properties, acting as antioxidant and antimicrobial agents.

scholarly journals EVALUATION OF THE CLINICAL EFFECTIVENESS OF TOOTHPASTE CONTAINING GRAPEFRUIT EXTRACT AND LYSOTECH AND PROTELYSE LYSATES IN THE COMPLEX TREATMENT OF INFLAMMATORY PERIODONTAL DISEASES

2021 ◽  
Vol 16 (4) ◽  
pp. 58-63
Author(s):  
Svetlana Tokmakova ◽  
Olga Bondarenko ◽  
Yuliya Lunitsyna
Keyword(s):  
Laboratory Study ◽  
Oral Hygiene ◽  
Therapeutic Potential ◽  
Inflammatory Diseases ◽  
Periodontal Diseases ◽  
Antibacterial Properties ◽  
Antimicrobial Properties ◽  
Complex Treatment ◽  
Periodontal Tissues

The preventive direction in dentistry is the leading one today. Individual oral hygiene plays a significant role in preventing the development of inflammatory periodontal diseases. The use of therapeutic and prophylactic toothpastes containing natural components with antibacterial properties is promising. Among plant extracts, grapefruit extract has the most pronounced antimicrobial activity. LysoTech and ProteLyse lysates, which have antimicrobial and immunomodulatory effects, have long been used in dentistry in the form of tablets for resorption in the complex treatment of various diseases. Their introduction into toothpastes is also considered a promising direction for the prevention and treatment of oral pathology. The aim of our study was to clinically evaluate the effectiveness of therapeutic and prophylactic toothpaste, which contains grapefruit extract and LysoTech and ProteLyse lysates, in patients with inflammatory diseases of periodontal tissues. A clinical and laboratory comparative study of two therapeutic and prophylactic toothpastes was conducted. The composition of the samples was identical, except for two components: grapefruit extract and LysoTech and ProteLyse lysates. The study involved 60 volunteers who were divided into two groups depending on the toothpastes used. The purifying and anti-inflammatory effects of the samples were evaluated for one month. An in vitro laboratory study was also conducted to identify the antimicrobial properties of toothpastes. During the work, high clinical results were noted in a group of volunteers using toothpaste with grapefruit seed extract and bacterial lysates, which are expressed in a decrease in PMA and SBI indices, and an improvement in oral hygiene. According to a laboratory study, the toothpaste containing grapefruit extract and LysoTech and ProteLyse lysates has a more pronounced antimicrobial and antifungal effect, which indicates a high preventive and therapeutic potential of the test sample.

One-Pot Three-Component Synthesis and Molecular Docking of Some Novel 2-Thiazolyl Pyridines as Potent Antimicrobial Agents

2019 ◽  
Vol 19 (6) ◽  
pp. 527-538 ◽  
Author(s):  
Fathy M. Abdelrazek ◽  
Sobhi M. Gomha ◽  
Mohamed E.B. Shaaban ◽  
Kamal A. Rabee ◽  
Heba N. El-Shemy ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Molecular Docking ◽  
Antimicrobial Agents ◽  
Wide Spectrum ◽  
Biological Effects ◽  
Binding Affinities ◽  
Thiazole Derivatives ◽  
One Pot ◽  
Three Component Reaction

Background: Thiazoles and pyridines are versatile synthetic scaffolds possessing wide spectrum of biological effects including potential antimicrobial activity. Objective: In the efforts to develop suitable antimicrobia drugs, medicinal chemists have focused on thiazole derivatives. A novel series of 2-thiazolyl pyridines was prepared in a one-pot three-component reaction using 2-bromoacetyl pyridine as a starting precursor. Method: Structure of the synthesized compounds was elucidated by spectral data (FT-IR, 1H NMR, 13C NMR, and mass) and elemental analyses. The prepared compounds were screened for their in vitro antimicrobial activity. Results: The results revealed that compounds 4a,b,e-g and 12 showed promising activity. Molecular docking studies using MOE software were carried out for compounds 4a and 4b which exhibited potent activities indicated by the diameter zones (4a; 3.6, 4.0, 1.2 mm) (4b; 4.2, 3.5, 1.5 mm) and the binding affinities (4a; -5.7731, -5.3576, -4.6844 kcal mol-1) (4b; -5.9356, -2.8250, -5.3628 kcal mol-1) against Candida albicans, Bacillus subtilis and Escherichia coli, respectively. Conclusion: This paper describes a facile and efficient MCR for synthesis of 2-thiazolyl pyridines from reaction of 2-bromoacetyl pyridine with different reagents. There was an agreement between the values of binding affinities and interactions and the data obtained from the practical antimicrobial screening of the tested compounds.

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