scholarly journals Antibacterial Activity of Thiazole and its Derivatives: A Review

2021 ◽  
Vol 12 (2) ◽  
pp. 2171-2195 ◽  
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Pharmaceutical Industry ◽  
Relevant Literature ◽  
Biological Significance ◽  
Antibacterial Properties ◽  
Molecular Probes ◽  
Thiazole Derivatives ◽  
Heterocyclic Derivatives ◽  
Significant Class

Thiazoles are one of the most intensively scrutinized classes of 5-membered aromatic heterocycles. Many natural and synthesized thiazole and its derivatives showed significant biological activity. Due to its unique properties, thiazole derivatives show significant antibacterial activity against various bacteria and pathogens. Thus, the present review ascribes the antibacterial activity of various thiazole and its derivatives. From using various databases, all the relevant literature has been reviewed. The review was deliberated based on the significant papers on the antibacterial activity of thiazole derivatives. Thiazole and its derivatives, a significant class of heterocyclic derivatives, have played an important role in chemical sciences. Due to their unique properties, they play an important role in the pharmaceutical industry. Thiazole and its derivatives show significant anticancer, anti-tuberculous, antioxidant, and anti-inflammatory activities. Due to their tremendous biological significance, scientists are actively engaged in designing new biological active thiazole derivatives. This review emphasized the antibacterial properties of various thiazole and its derivatives. The present study will help researchers design and synthesize various biological active molecular probes and study their antibacterial properties using various processes against various bacteria and pathogens.

scholarly journals The Antibacterial Activity and Phytochemical Compounds of Citrus grandis Extract Against Human Infective Bacteria

2020 ◽  
Vol 24 (3) ◽  
Author(s):  
Mostafa Alamholo ◽  
Mohaddeseh Shojaemehr
Keyword(s):  
Antibacterial Activity ◽  
Pharmaceutical Industry ◽  
Secondary Metabolites ◽  
Pathogenic Bacteria ◽  
Methanol Extract ◽  
Antibacterial Properties ◽  
Diffusion Method ◽  
Total Phenol Content ◽  
White Skin ◽  
Phytochemical Compounds

Background: With the presence of secondary metabolites that have antimicrobial properties and bacterial resistance against antibiotics, medicinal plants have attracted the attention of researchers in the pharmaceutical industry. Objectives: The present study aimed to investigate the antibacterial and antioxidant activity and phytochemical compounds of Citrus grandis extract against human infection bacteria in-vitro. Methods: Samples of Citrus grandis were collected from the north of Iran and assessed in terms of the antibacterial activity, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) using the agar well diffusion method. In addition, the anti-radical activity was determined by DPPH, total phenols were measured using the Folin-Ciocalteu method, and flavonoids were determined using aluminum chloride. The presence of alkaloid, saponin, and tannin was also investigated. Data analysis was performed in SPSS. Results: The colored and white skin methanol extract of C. grandis indicated more significant inhibitory effects on Bacillus cereus, Staphylococcus aureus, and Micrococcus luteus. The total phenol content of the colored and white skin was estimated at 79.71 and 71.63 mgGA/g, and the flavonoid level was determined to be 3.63 and 4.06 mgQ/g, respectively. The IC50 of the colored and white skin methanol extract and ascorbic acid were estimated at 0.1251, 0.1376, and 0.1095 mg.mL-1, respectively. The methanol extract of the colored skin showed the presence of alkaloid, while the white skin showed the presence of alkaloid and saponin. Conclusions: According to the results, the C. grandis extract had antioxidant and antibacterial properties due to the presence of secondary metabolites. Therefore, it is recommended that natural and rare drugs be produced to control pathogenic bacteria in the pharmaceutical industry.

Complexes of Cu (II) with a-Ketoglutaric Acid and 1- (o-tolyl) Biguanide Synthesis, characterization and biological Activity

2019 ◽  
Vol 70 (10) ◽  
pp. 3603-3610
Author(s):  
Madalina Mihalache ◽  
Cornelia Guran ◽  
Aurelia Meghea ◽  
Vasile Bercu ◽  
Ludmila Motelica ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Biological Activity ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Copper Complexes ◽  
Substrate Adhesion ◽  
Inert Substrate

The three copper complexes having a-ketoglutaric acid (H2A) and 1- (o-tolyl) biguanide (TB) ligands have been synthesized and characterized. The proposed formulas for these complexes are: [Cu(TB)(HA)]Cl (C1), [Cu(TB)(HA)CH3COO]�H2O (C2) and [Cu(TB)(HA)](NO3) (C3) where HA represents deprotonated H2A. The complexes obtained were tested for antibacterial activity against Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853, antifungal activity on Candida albicans ATCC 10231 and antitumor activity on HeLa tumor cells. Due to the antitumor, antifungal, antimicrobial activity and inhibition of inert substrate adhesion, complexes synthesized could be used for potential therapeutic applications.

Review: Studies on the Synthesis of Quinolone Derivatives with Their Antibacterial Activity (Part 1)

2020 ◽  
Vol 24 (8) ◽  
pp. 817-854
Author(s):  
Anil Kumar ◽  
Nishtha Saxena ◽  
Arti Mehrotra ◽  
Nivedita Srivastava
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Properties ◽  
Structure Activity Relationship ◽  
New Drugs ◽  
Activity Relationship ◽  
Structure Activity ◽  
Medicinal Properties ◽  
Synthetic Routes ◽  
Quinolone Derivatives

Quinolone derivatives have attracted considerable attention due to their medicinal properties. This review covers many synthetic routes of quinolones preparation with their antibacterial properties. Detailed study with structure-activity relationship among quinolone derivatives will be helpful in designing new drugs in this field.

Fluoroquinolone-3-carboxamide Amino Acid Conjugates: Synthesis, Antibacterial Properties And Molecular Modeling Studies

2020 ◽  
Vol 17 (1) ◽  
pp. 71-84
Author(s):  
Riham M. Bokhtia ◽  
Siva S. Panda ◽  
Adel S. Girgis ◽  
Hitesh H. Honkanadavar ◽  
Tarek S. Ibrahim ◽  
...  
Keyword(s):  
Experimental Data ◽  
Antibacterial Activity ◽  
Amino Acid ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Antibacterial Properties ◽  
Computational Studies ◽  
Protecting Group ◽  
Amino Acid Conjugates ◽  
Molecular Modeling Studies

Background: Bacterial infections are considered as one of the major global health threats, so it is very essential to design and develop new antibacterial agents to overcome the drawbacks of existing antibacterial agents. Method: The aim of this work is to synthesize a series of new fluoroquinolone-3-carboxamide amino acid conjugates by molecular hybridization. We utilized benzotriazole chemistry to synthesize the desired hybrid conjugates. Result: All the conjugates were synthesized in good yields, characterized, evaluated for their antibacterial activity. The compounds were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Synthesized conjugates were tested for activity against medically relevant pathogens; Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27856) Staphylococcus aureus (ATCC 25923) and Enterococcus faecalis (ATCC 19433). Conclusion: The observed antibacterial experimental data indicates the selectivity of our synthesized conjugates against E.Coli. The protecting group on amino acids decreases the antibacterial activity. The synthesized conjugates are non-toxic to the normal cell lines. The experimental data were supported by computational studies.

Biological Activity of Thiazole Derivatives on Some Pathogenic Microorganisms

2011 ◽  
Vol 14 (1) ◽  
pp. 1-6
Author(s):  
Firas A. Hassan ◽  
◽  
Zahraa. S. Saeed ◽  
Shayma M. Ahmad ◽  
◽  
...  
Keyword(s):  
Biological Activity ◽  
Pathogenic Microorganisms ◽  
Thiazole Derivatives

scholarly journals New Mononuclear and Binuclear Cu(II), Co(II), Ni(II), and Zn(II) Thiosemicarbazone Complexes with Potential Biological Activity: Antimicrobial and Molecular Docking Study

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2288
Author(s):  
Ahmed Gaber ◽  
Moamen S. Refat ◽  
Arafa A.M. Belal ◽  
Ibrahim M. El-Deen ◽  
Nader Hassan ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Molecular Docking ◽  
Metal Complexes ◽  
Analytical Data ◽  
Docking Study ◽  
Spectroscopic Techniques ◽  
Molecular Docking Study ◽  
Tetrahedral Geometry ◽  
Thiosemicarbazone Complexes

Herein, we report the synthesis of eight new mononuclear and binuclear Co2+, Ni2+, Cu2+, and Zn2+ methoxy thiosemicarbazone (MTSC) complexes aiming at obtaining thiosemicarbazone complex with potent biological activity. The structure of the MTSC ligand and its metal complexes was fully characterized by elemental analysis, spectroscopic techniques (NMR, FTIR, UV-Vis), molar conductivity, thermogravimetric analysis (TG), and thermal differential analysis (DrTGA). The spectral and analytical data revealed that the obtained thiosemicarbazone-metal complexes have octahedral geometry around the metal center, except for the Zn2+-thiosemicarbazone complexes, which showed a tetrahedral geometry. The antibacterial and antifungal activities of the MTSC ligand and its (Co2+, Ni2+, Cu2+, and Zn2+) metal complexes were also investigated. Interestingly, the antibacterial activity of MTSC- metal complexes against examined bacteria was higher than that of the MTSC alone, which indicates that metal complexation improved the antibacterial activity of the parent ligand. Among different metal complexes, the MTSC- mono- and binuclear Cu2+ complexes showed significant antibacterial activity against Bacillus subtilis and Proteus vulgaris, better than that of the standard gentamycin drug. The in silico molecular docking study has revealed that the MTSC ligand could be a potential inhibitor for the oxidoreductase protein.

scholarly journals Differential Role of Threonine and Tyrosine Phosphorylation in the Activation and Activity of the Yeast MAPK Slt2

2021 ◽  
Vol 22 (3) ◽  
pp. 1110
Author(s):  
Gema González-Rubio ◽  
Ángela Sellers-Moya ◽  
Humberto Martín ◽  
María Molina
Keyword(s):  
Cell Wall ◽  
Biological Activity ◽  
Biological Significance ◽  
Mitogen Activated Protein Kinase ◽  
Activation Loop ◽  
High Increase ◽  
Dual Specificity ◽  
Mitogen Activated Protein ◽  
Full Activation

The Mitogen-Activated Protein Kinase (MAPK) Slt2 is central to signaling through the yeast Cell Wall Integrity (CWI) pathway. MAPKs are regulated by phosphorylation at both the threonine and tyrosine of the conserved TXY motif within the activation loop (T190/Y192 in Slt2). Since phosphorylation at both sites results in the full activation of MAPKs, signaling through MAPK pathways is monitored with antibodies that detect dually phosphorylated forms. However, most of these antibodies also recognize monophosphorylated species, whose relative abundance and functionality are diverse. By using different phosphospecific antibodies and phosphate-affinity (Phos-tag) analysis on distinct Slt2 mutants, we determined that Y192- and T190-monophosphorylated species coexist with biphosphorylated Slt2, although most of the Slt2 pool remains unphosphorylated following stress. Among the monophosphorylated forms, only T190 exhibited biological activity. Upon stimulation, Slt2 is first phosphorylated at Y192, mainly by the MAPKK Mkk1, and this phosphorylation is important for the subsequent T190 phosphorylation. Similarly, dephosphorylation of Slt2 by the Dual Specificity Phosphatase (DSP) Msg5 is ordered, with dephosphorylation of T190 depending on previous Y192 dephosphorylation. Whereas Y192 phosphorylation enhances the Slt2 catalytic activity, T190 is essential for this activity. The conserved T195 residue is also critical for Slt2 functionality. Mutations that abolish the activity of Slt2 result in a high increase in inactive Y192-monophosphorylated Slt2. The coexistence of different Slt2 phosphoforms with diverse biological significance highlights the importance of the precise detection of the Slt2 phosphorylation status.

scholarly journals Antibacterial Activity of Moroccan Zantaz Honey and the Influence of Its Physicochemical Parameters Using Chemometric Tools

2021 ◽  
Vol 11 (10) ◽  
pp. 4675
Author(s):  
Youssef Elamine ◽  
Hamada Imtara ◽  
Maria Graça Miguel ◽  
Ofélia Anjos ◽  
Letícia M. Estevinho ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Properties ◽  
Principal Component ◽  
Physicochemical Characteristics ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Coumaric Acid ◽  
Atlas Mountains ◽  
Methyl Syringate ◽  
Chemometric Tools

The emergence of multidrug-resistant bacteria has prompted the development of alternative therapies, including the use of natural products with antibacterial properties. The antibacterial properties of Zantaz honey produced in the Moroccan Atlas Mountains against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus was evaluated and analyzed using chemometric tools. Minimum inhibitory concentration (MIC) and Minimum bactericidal concentration (MBC) against S. aureus were the lowest (112.5 ± 54.5 mg/mL), revealing that this species was most sensitive to Zantaz honey. P. aeruginosa showed an intermediate sensitivity (MIC= 118.75 ± 51.9 mg/mL), while E. coli was the most resistant to treatment (MIC = 175 ± 61.2 mg/mL). Content of monosaccharides, certain minerals, and phenolic compounds correlated with antibacterial activity (p < 0.05). Principal component analysis of physicochemical characteristics and antibacterial activity indicated that the parameters most associated with antibacterial activity were color, acidity, and content of melanoidins, fructose, epicatechin, methyl syringate, 4-coumaric acid, and 3-coumaric acid.

Bicomponent multifilament yarns of recycled poly(ethylene terephthalate) and nano-titanium dioxide for antibacterial carpet

2021 ◽  
pp. 152808372110117
Author(s):  
Sommai Pivsa-Art ◽  
Komson Sunyikhan ◽  
Weraporn Pivsa-Art
Keyword(s):  
Antibacterial Activity ◽  
Titanium Dioxide ◽  
Ethylene Terephthalate ◽  
Antibacterial Properties ◽  
Nano Structure ◽  
Elongation At Break ◽  
High Antibacterial Activity ◽  
Poly Ethylene Terephthalate ◽  
Poly Ethylene ◽  
Multifilament Yarns

Recycled poly(ethylene terephthalate) (RPET) multifilament yarns are used in carpet manufacturing as a way to reduce plastic waste. The conventional RPET carpet is however susceptible to bacterial accumulation. As a result, this research experimentally doped RPET with nano-structure titanium dioxide (nano-TiO2) to produce RPET/nano-TiO2 bicomponent multifilament yarns with antibacterial property. The experimental multifilament yarn structure consisted of two parts: neat RPET core and RPET/nano-TiO2 shell. The nano-TiO2 content in the shell was varied between 1 and 3 wt% and the core/shell (C/S) ratios between 90/10, 70/30, and 50/50 w/w. The effects of C/S ratio and nano-TiO2 content on the mechanical and antibacterial properties of bicomponent multifilament yarns were determined. The experimental results indicated that the C/S ratio had no effect on the tenacity and elongation at break. Meanwhile, the tenacity and elongation at break of bicomponent fibers increased with nano-TiO2 content in the shell. The TiO2-doped RPET bicomponent yarns effectively inhibited the growth of Escherichia coli and Staphylococcus aureus. The 90/10 bicomponent multifilament fiber with 3 wt% TiO2 achieved the highest antibacterial activity. The very high antibacterial activity was attributable to greater deposition of nano-TiO2 particles near and on the shell surface.

scholarly journals In Vitro Anti-Biofilm and Antibacterial Properties of Streptococcus downii sp. nov.

2021 ◽  
Vol 9 (2) ◽  
pp. 450
Author(s):  
Maigualida Cuenca ◽  
María Carmen Sánchez ◽  
Pedro Diz ◽  
Lucía Martínez-Lamas ◽  
Maximiliano Álvarez ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Quantitative Polymerase Chain Reaction ◽  
Bacterial Load ◽  
Antibacterial Properties ◽  
Antibacterial Activities ◽  
Oral Bacteria ◽  
Periodontal Pathogens ◽  
Biofilm Model ◽  
Biofilm Development

The aim of this study was to evaluate the potential anti-biofilm and antibacterial activities of Streptococcus downii sp. nov. To test anti-biofilm properties, Streptococcus mutans, Actinomyces naeslundii, Veillonella parvula, Fusobacterium nucleatum, Porphyromonas gingivalis, and Aggregatibacter actinomycetemcomitans were grown in a biofilm model in the presence or not of S. downii sp. nov. for up to 120 h. For the potential antibacterial activity, 24 h-biofilms were exposed to S. downii sp. nov for 24 and 48 h. Biofilms structures and bacterial viability were studied by microscopy, and the effect in bacterial load by quantitative polymerase chain reaction. A generalized linear model was constructed, and results were considered as statistically significant at p < 0.05. The presence of S. downii sp. nov. during biofilm development did not affect the structure of the community, but an anti-biofilm effect against S. mutans was observed (p < 0.001, after 96 and 120 h). For antibacterial activity, after 24 h of exposure to S. downii sp. nov., counts of S. mutans (p = 0.019) and A. actinomycetemcomitans (p = 0.020) were significantly reduced in well-structured biofilms. Although moderate, anti-biofilm and antibacterial activities of S. downii sp. nov. against oral bacteria, including some periodontal pathogens, were demonstrated in an in vitro biofilm model.

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