scholarly journals Microwave Mediated Synthesis of Novel 1,3,5-Triazine Derivative and their Biological Evaluation

2021 ◽  
Vol 3 (12) ◽  
pp. 181-185
Author(s):  
Krishn Kumar Barmase ◽  
Deepak Basedia ◽  
Balkrishna Dubey
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Effect ◽  
Bacterial Species ◽  
Biological Evaluation ◽  
Chloride Ions ◽  
Gram Negative ◽  
Triazine Derivative ◽  
Triazine Derivatives ◽  
In Vitro Antibacterial Activity

1,3,5-Triazine derivative are synthesized by replacement of chloride ions of Cyanuric chloride and 1,3,5-Triazine derivative are showing promising biologically activity such as Antibacterial, Antifungal, Antimalarial, Antivirus, Anticancer that’s why interest of researches on synthesis of 1,3,5-Triazine derivatives always in focused. The present study reported the synthesis of 2,4,6-Trisubstituted 1,3,5-Triazine derivatives by Microwave mediated Method which gave the desired result in less time with higher yield. The structure of 1,3,5-Triazine derivatives have been elucidated by Spectral of IR, NMR and MASS. The derivative of 1,3,5-Triazine are evaluated for their In vitro Antibacterial activity against Gram Positive and Gram Negative Bacterial species and shown good Antibacterial effect.

scholarly journals In vitro antibacterial activity of essential oils from Lamiaceae species

2016 ◽  
Vol 5 (4) ◽  
pp. 141-144
Author(s):  
Vinod Kumar ◽  
◽  
C. S. Mathela ◽  
Amit Panwar ◽  
◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Essential Oils ◽  
Broad Spectrum ◽  
Antibacterial Effect ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Gram Negative ◽  
In Vitro Antibacterial Activity

Essential oils from Calamintha umbrosa and Nepeta species viz. N. leucophylla; N. hindostana; N. ciliaris and N. clarkei (family Lamiaceae), was tested against six bacterial strains. To evaluate the correlation between the antimicrobial activity and the essential oils, PCA and HCA analysis was done. PCA and HCA analysis of the antibacterial activity revealed that essential oils of Nepeta species had a strong and broad spectrum antibacterial effect against bacterial strains of P. aeruginosa and S. scandidus. The N. leucophylla oil showed higher activity against Gram-negative bacteria P. aeruginosa (10.5 mm, MIC 10 µL/mL) and K. pneumonia (9.1 mm, MIC 45 µL/mL) among all Nepeta oils which may be due to presence of active antimicrobial iridoids compounds.

scholarly journals Chemical Composition and in Vitro Antibacterial Activity of the Essential Oil of Minthostachys Mollis (Kunth) Griseb Vaught from the Venezuelan Andes

2009 ◽  
Vol 4 (7) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Flor D. Mora ◽  
María Araque ◽  
Luis B. Rojas ◽  
Rosslyn Ramírez ◽  
Bladimiro Silva ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Essential Oil ◽  
Chemical Constituents ◽  
Salmonella Typhi ◽  
Inhibitory Effect ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Significant Inhibitory Effect ◽  
In Vitro Antibacterial Activity

Chemical constituents of the essential oil from the leaves of Minthostachys mollis (Kunth) Griseb Vaught var. mollis collected in January 2008 at Tuñame, Trujillo State, Venezuela, were separated and identified by GCMS analysis. The essential oil was obtained by hydrodistillation and thirteen components (98.5% of the sample) were identified by comparison with the Wiley GCMS library data base. The two major components were pulegone (55.2%) and trans-menthone (31.5%). The essential oil showed a significant inhibitory effect against Gram-positive and Gram-negative bacteria, especially Bacillus subtilis and Salmonella typhi (4 μg/mL).

scholarly journals In VitroAntibacterial Activity of AZD0914, a New Spiropyrimidinetrione DNA Gyrase/Topoisomerase Inhibitor with Potent Activity against Gram-Positive, Fastidious Gram-Negative, and Atypical Bacteria

2014 ◽  
Vol 59 (1) ◽  
pp. 467-474 ◽  
Author(s):  
Michael D. Huband ◽  
Patricia A. Bradford ◽  
Linda G. Otterson ◽  
Gregory S. Basarab ◽  
Amy C. Kutschke ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Legionella Pneumophila ◽  
Bacterial Species ◽  
Dna Gyrase ◽  
Cross Resistance ◽  
Gram Positive ◽  
Gram Negative ◽  
Content Type ◽  
Topoisomerase Inhibitor

ABSTRACTAZD0914 is a new spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor with potentin vitroantibacterial activity against key Gram-positive (Staphylococcus aureus,Staphylococcus epidermidis,Streptococcus pneumoniae,Streptococcus pyogenes, andStreptococcus agalactiae), fastidious Gram-negative (Haemophilus influenzaeandNeisseria gonorrhoeae), atypical (Legionella pneumophila), and anaerobic (Clostridium difficile) bacterial species, including isolates with known resistance to fluoroquinolones. AZD0914 works via inhibition of DNA biosynthesis and accumulation of double-strand cleavages; this mechanism of inhibition differs from those of other marketed antibacterial compounds. AZD0914 stabilizes and arrests the cleaved covalent complex of gyrase with double-strand broken DNA under permissive conditions and thus blocks religation of the double-strand cleaved DNA to form fused circular DNA. Whereas this mechanism is similar to that seen with fluoroquinolones, it is mechanistically distinct. AZD0914 exhibited low frequencies of spontaneous resistance inS. aureus, and if mutants were obtained, the mutations mapped togyrB. Additionally, no cross-resistance was observed for AZD0914 against recent bacterial clinical isolates demonstrating resistance to fluoroquinolones or other drug classes, including macrolides, β-lactams, glycopeptides, and oxazolidinones. AZD0914 was bactericidal in both minimum bactericidal concentration andin vitrotime-kill studies. Inin vitrocheckerboard/synergy testing with 17 comparator antibacterials, only additivity/indifference was observed. The potentin vitroantibacterial activity (including activity against fluoroquinolone-resistant isolates), low frequency of resistance, lack of cross-resistance, and bactericidal activity of AZD0914 support its continued development.

Catalyst Free and Energy Economical Synthesis of Thiazole Derivatives Bearing Azo Imine Linkage with Imidazole as Antimicrobial Agents

2019 ◽  
Vol 16 (3) ◽  
pp. 284-290
Author(s):  
Nayan M. Panchani ◽  
Hitendra S. Joshi
Keyword(s):  
Antibacterial Activity ◽  
Room Temperature ◽  
Antimicrobial Agents ◽  
Fungal Infections ◽  
Gram Negative Bacteria ◽  
Thiazole Derivatives ◽  
Microbial Diseases ◽  
Gram Negative ◽  
In Vitro Antibacterial Activity

Background:Several strategies have been reported for the synthesis of thiazole derivatives.Methods:However, many of these methods suffer from several drawbacks. Several modifications have been made to counter these problems. Here, we have synthesized a new series of 2-(2-((1HImidazol- 4-yl)methylene)hydrazinyl)-4-(4-substitutedphenyl)thiazoles without using the catalyst at room temperature.Results:The structures of synthesized compounds have been confirmed by spectral analysis, such as Mass, IR, 1H NMR and 13C NMR. All synthesized compounds were screened for in vitro antibacterial activity against some gram-positive and gram-negative bacteria.Conclusion:The thiazole derivatives, with a pharmacologically potent group, discussed in this article may provide valued therapeutic important in the treatment of microbial diseases, especially against bacterial and fungal infections.

scholarly journals Synthesis and Biological Evaluation of New Pyridothienopyrimidine Derivatives as Antibacterial Agents and Escherichia coli Topoisomerase II Inhibitors

Antibiotics ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 695
Author(s):  
Eman M. Mohi El-Deen ◽  
Eman A. Abd El-Meguid ◽  
Eman A. Karam ◽  
Eman S. Nossier ◽  
Marwa F. Ahmed
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Topoisomerase Ii ◽  
Antibacterial Agents ◽  
Dna Gyrase ◽  
Structural Features ◽  
Biological Evaluation ◽  
Topoisomerase Iv ◽  
Gram Negative

The growing resistance of bacteria to many antibiotics that have been in use for several decades has generated the need to discover new antibacterial agents with structural features qualifying them to overcome the resistance mechanisms. Thus, novel pyridothienopyrimidine derivatives (2a,b–a,b) were synthesized by a series of various reactions, starting with 3-aminothieno[2,3-b]pyridine-2-carboxamides (1a,b). Condensation of compounds 1a,b with cyclohexanone gave 1’H-spiro[cyclohexane-1,2’-pyrido[3’,2’:4,5]thieno[3,2-d]pyrimidin]-4’(3’H)-ones (2a,b), which in turn were utilized to afford the target 4-substituted derivatives (3a,b–8a,b). In vitro antibacterial activity evaluations of all the new compounds (2a,b–8a,b) were performed against six strains of Gram-negative and Gram-positive bacteria. The target compounds showed significant antibacterial activity, especially against Gram-negative strains. Moreover, the compounds (2a,b; 3a,b; 4a,b; and 5a,b) that exhibited potent activity against Escherichia coli were selected to screen their inhibitory activity against Escherichia coli topoisomerase II (DNA gyrase and topoisomerase IV) enzymes. Compounds 4a and 4b showed potent dual inhibition of the two enzymes with IC50 values of 3.44 µΜ and 5.77 µΜ against DNA gyrase and 14.46 µΜ and 14.89 µΜ against topoisomerase IV, respectively. In addition, docking studies were carried out to give insight into the binding mode of the tested compounds within the E. coli DNA gyrase B active site compared with novobiocin.

Sign in / Sign up

Export Citation Format

Share Document