scholarly journals Synthesis, Anti-microbial, Flameretardance and Anti-corrosive Activity of Some New Heterocycles Incorporating Coumarin moiety

2020 ◽  
pp. 23-37
Author(s):  
S. M. Mohamed ◽  
Nadia T. A. Dawoud ◽  
N. Abd El-Khalik ◽  
Wafaa. M. Mazen ◽  
Z. I. El Bailey
Keyword(s):  
Heterocyclic Compounds ◽  
Gram Negative Bacteria ◽  
Coumarin Derivatives ◽  
Flame Resistance ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
In Vitro Antibacterial Activity ◽  
Flame Retardant Properties ◽  
Corrosive Activity

In the present study a series of novel heterocyclic compounds (2-16) incorporating coumarin moiety was synthesized. The newly synthesized compounds were elucidated on the basis of elemental analysis, spectral data, were tested for in-vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis (Gram-positive bacteria), Salmonella typhimurium, Escherichia coli (Gram-negative bacteria) and Candida albicans, Aspergillus fumigatus (fungi). Coumarin derivatives (1,6,16) were chosen to evaluate the anti-corrosion, flame retardant properties. The results clearly showed that, the incorporation of coumarin derivatives into epoxy coating have led to improve the flame residency, corrosion resistance, and mechanical properties of investigated coating and confirmed that these new developed varnishes have an excellent properties as flame resistance and anticorrosive for mild steel.

Synthesis and Antimicrobial Evaluation of 1,3,4-Oxadiazole bearing Schiff Base Moiety

2020 ◽  
Vol 5 (1) ◽  
pp. 1-5
Author(s):  
K. Kapadiya ◽  
G. Dubal ◽  
Y. Bhola ◽  
P. Dholaria
Keyword(s):  
Streptococcus Pyogenes ◽  
Nmr Spectra ◽  
Gram Negative Bacteria ◽  
13C Nmr Spectra ◽  
Aspergillus Clavatus ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
In Vitro Antibacterial Activity ◽  
Antimicrobial Evaluation

A new series of 4-((5-(2-chlorophenyl)-1,3,4-oxadiazol-2-yl)methoxy)-N-(benzylidene derivatives)benzenamine (5a-k) have been synthesized and were screened for their in vitro antibacterial activity against Gram-positive bacteria (Pseudomonas aeruginosa, Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli, Staphylococcus aureus) and antifungal activity (Candida albicans, Aspergillus niger, Aspergillus clavatus). Synthesized compounds were characterized by IR, mass (MS), 1H NMR and 13C NMR spectra. The synthesized compounds 5b, 5c, 5g and 5i showed potency in terms of antimicrobial activity against tested microorganisms.

scholarly journals Synthesis and antibacterial studies of some novel isoxazoline derivatives

2007 ◽  
Vol 72 (5) ◽  
pp. 443-449 ◽  
Author(s):  
Tejaskumar Shah ◽  
Vikas Desai
Keyword(s):  
Antibacterial Activity ◽  
Spectral Data ◽  
Elemental Analysis ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Antibacterial Studies ◽  
In Vitro Antibacterial Activity

A series of 3-[3-(2,4-dichloro-5-fluorophenyl)-5-(2-furyl)-4,5-dihydro-1H-pyrazol- 1-yl]-5-(substituted phenyl/2-thienyl)isoxazolines (4a-j) were prepared. The structures of the isoxazoline derivatives were confirmed on the bases of elemental analysis and spectral data. The compounds were screened for their in vitro antibacterial activity using gram-positive bacteria and gram-negative bacteria.

scholarly journals In Vitro and In Vivo Antibacterial Activities of DW-224a, a New Fluoronaphthyridone

2006 ◽  
Vol 50 (6) ◽  
pp. 2261-2264 ◽  
Author(s):  
Hee-Soo Park ◽  
Hyun-Joo Kim ◽  
Min-Jung Seol ◽  
Dong-Rack Choi ◽  
Eung-Chil Choi ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
The Other ◽  
Vitro Activity ◽  
Gram Negative Bacteria ◽  
In Vitro Activity ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria

ABSTRACT DW-224a showed the most potent in vitro activity among the quinolone compounds tested against clinical isolates of gram-positive bacteria. Against gram-negative bacteria, DW-224a was slightly less active than the other fluoroquinolones. The in vivo activities of DW-224a against gram-positive bacteria were more potent than those of other quinolones.

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 Vitro Activities of ME1036 (CP5609), a Novel Parenteral Carbapenem, against Methicillin-Resistant Staphylococci

2004 ◽  
Vol 48 (8) ◽  
pp. 2831-2837 ◽  
Author(s):  
Mizuyo Kurazono ◽  
Takashi Ida ◽  
Keiko Yamada ◽  
Yoko Hirai ◽  
Takahisa Maruyama ◽  
...  
Keyword(s):  
Multiple Drug ◽  
Gram Negative Bacteria ◽  
Coagulase Negative Staphylococci ◽  
Gram Positive ◽  
Gram Negative ◽  
Methicillin Resistant ◽  
Gram Positive Bacteria ◽  
Multiple Drug Resistant ◽  
Time Kill

ABSTRACT ME1036, formerly CP5609, is a novel parenteral carbapenem with a 7-acylated imidazo[5,1-b]thiazole-2-yl group directly attached to the carbapenem moiety of the C-2 position. The present study evaluated the in vitro activities of ME1036 against clinical isolates of gram-positive and gram-negative bacteria. ME1036 displayed broad activity against aerobic gram-positive and gram-negative bacteria. Unlike other marketed β-lactam antibiotics, ME1036 maintained excellent activity against multiple-drug-resistant gram-positive bacteria, such as methicillin-resistant staphylococci and penicillin-resistant Streptococcus pneumoniae (PRSP). The MICs of this compound at which 90% of isolates were inhibited were 2 μg/ml for methicillin-resistant Staphylococcus aureus (MRSA), 2 μg/ml for methicillin-resistant coagulase-negative staphylococci, and 0.031 μg/ml for PRSP. In time-kill studies with six strains of MRSA, ME1036 at four times the MIC caused a time-dependent decrease in the numbers of viable MRSA cells. The activity of ME1036 against MRSA is related to its high affinity for penicillin-binding protein 2a, for which the 50% inhibitory concentration of ME1036 was approximately 300-fold lower than that of imipenem. In conclusion, ME1036 demonstrated a broad antibacterial spectrum and high levels of activity in vitro against staphylococci, including β-lactam-resistant strains.

scholarly journals Amidoalkylation of heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]- 2'-chloroacetamide and antimicrobial activity of derivatives

2021 ◽  
Vol 10 (4) ◽  
pp. 427-434 ◽  
Author(s):  
Turdibek Toshmurodov ◽  
Abdukhakim Ziyaev ◽  
Sobirdjan Sasmakov ◽  
Jaloliddin Abdurakhmanov ◽  
Mavluda Ziyaeva ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Inhibition Zone ◽  
Heterocyclic Amines ◽  
Gram Negative Bacteria ◽  
In Vitro Screening ◽  
Gram Negative ◽  
Inhibition Zone Diameter ◽  
Gram Positive Bacteria ◽  
New Compounds

Amidoalkylation of secondary heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-chloroacetamide resulted the new compounds 5-10 that contain 1,3,4-thiadiazole-5-thione moiety alongside pyperidine, morpholine, and cytisine fragments. In vitro screening of antimicrobial activity of synthesized compounds showed that N-[5-(amylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-morpholinacetamide exhibited an appreciable antibacterial activity against gram-negative bacteria of Escherichia coli (inhibition zone diameter of 16 mm) and gram-positive bacteria of Staphylococcus aureus and Bacillus subtilis (10-13 mm).

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 Bacterial Induction of Beta Interferon in Mice Is a Function of the Lipopolysaccharide Component

2000 ◽  
Vol 68 (3) ◽  
pp. 1600-1607 ◽  
Author(s):  
Andreas Sing ◽  
Thomas Merlin ◽  
Hans-Peter Knopf ◽  
Peter J. Nielsen ◽  
Harald Loppnow ◽  
...  
Keyword(s):  
Mouse Strains ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Necrosis Factor Alpha ◽  
Gram Negative ◽  
Protein Levels ◽  
Gram Positive Bacteria ◽  
Beta Interferon

ABSTRACT We investigated the reason for the inability of lipopolysaccharide (LPS)-resistant (Lps-defective [Lpsd ]) C57BL/10ScCr mice to produce beta interferon (IFN-β) when stimulated with bacteria. For this purpose, the IFN-β and other macrophage cytokine responses induced by LPS and several killed gram-negative and gram-positive bacteria in LPS-sensitive (Lps-normal [Lpsn ]; C57BL/10ScSn and BALB/c) and Lpsd (C57BL/10ScCr and BALB/c/l) mice in vitro and in vivo were investigated on the mRNA and protein levels. In addition, double-stranded RNA (dsRNA) was used as a nonbacterial stimulus. LPS and all gram-negative bacteria employed induced IFN-β in the Lpsn mice but not in theLpsd mice. All gram-positive bacteria tested failed to induce significant amounts of IFN-β in all four of the mouse strains used. As expected, all other cytokines tested (tumor necrosis factor alpha, interleukin 1α [IL-1α], IL-6, and IL-10) were differentially induced by gram-negative and gram-positive bacteria. Stimulation with dsRNA induced IFN-β and all other cytokines mentioned above in all mouse strains, regardless of their LPS sensitivities. The results suggest strongly that LPS is the only bacterial component capable of inducing IFN-β in significant amounts that are readily detectable under the conditions used in this study. Consequently, in mice, IFN-β is inducible only by gram-negative bacteria, but not in C57BL/10ScCr or other LPS-resistant mice.

scholarly journals A Xenorhabdus budapestensis entomopatogén baktérium sejtmentes fermentlevének és tisztítottfehérje-frakciójának antimikrobiális hatása néhány zoonoticus baktériumra

2015 ◽  
Vol 156 (44) ◽  
pp. 1782-1786 ◽  
Author(s):  
Erzsébet Burgettiné Böszörményi ◽  
István Barcs ◽  
Gyula Domján ◽  
Katalin Bélafiné Bakó ◽  
András Fodor ◽  
...  
Keyword(s):  
Pasteurella Multocida ◽  
Antibacterial Effect ◽  
Conditioned Media ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Salmonella Gallinarum ◽  
Gram Positive Bacteria ◽  
Agar Diffusion Test

Introduction: Many multi-resistant patogens appear continuously resulting in a permanent need for the development of novel antibiotics. A large number of antibiotics introduced in clinical and veterinary practices are not effective. Antibacterial peptides with unusual mode of action may represent a promising option against multi-resistant pathogens. The entomopathogenic Xenorhabdus budapestensis bacteria produce several different antimicrobial peptides compounds such as bicornutin-A and fabclavin. Aim: The aim of the authors was to evaluate the in vitro antibacterial effect of Xenorhabdus budapestensis using zoonotic patogen bacteria. Method: Cell-free conditioned media and purified peptide fractions of Xenorhabdus budapestensis were tested on Gram-positive (Rhodococcus equi, Erysipelothrix rhusiopathia, Staphylococcus aureus, Streptococcus equi, Corynebacterium pseudotuberculosis, Listeria monocytagenes) and Gram-negative bacteria (Salmonella gallinarum, Salmonella derbi, Bordatella bronchoseptica, Escherichia coli, Pasteurella multocida, Aeromonas hydrophila) using agar diffusion test on blood agar plates. Results: It was found that Xenorhabdus budapestensis bacteria produced compounds with strong and dose-dependent effects on the tested organisms. Purified peptid fraction exerted a more marked effect than cell free conditioned media. Gram-positive bacteria were more sensitive to this antibacterial effect than Gram-negative bacteria. Conclusions: Antibacterial peptide compound from Xenorhabdus budapestensis exert marked antibacterial effect on zoonotic patogen bacteria and they should be further evaluated in future for their potential use in the control or prevention of zoonoses. Orv. Hetil., 2015, 156(44), 1782–1786.

scholarly journals In Vitro and In Vivo Antibacterial Activities of DW286, a New Fluoronaphthyridone Antibiotic

2002 ◽  
Vol 46 (9) ◽  
pp. 3071-3074 ◽  
Author(s):  
Hee-Jeong Yun ◽  
Yu-Hong Min ◽  
Jung-A Lim ◽  
Jin-Wook Kang ◽  
So-Young Kim ◽  
...  
Keyword(s):  
Staphylococcus Epidermidis ◽  
Systemic Infection ◽  
Antibacterial Activities ◽  
The Other ◽  
Gram Negative Bacteria ◽  
In Vitro Activity ◽  
Gram Negative ◽  
Gram Positive Bacteria

ABSTRACT The in vitro and in vivo activities of DW286, a novel fluoronaphthyridone with potent antibacterial activity, were compared with those of ciprofloxacin, gemifloxacin, sparfloxacin, and trovafloxacin. Against gram-positive bacteria, such as Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, and Enterococcus faecalis, the in vitro activity of DW286 was stronger than that of any other reference antibiotic. Against gram-negative bacteria, the activity of DW286 was similar to those of trovafloxacin and gemifloxacin but was weaker than that of ciprofloxacin. In a mouse systemic infection caused by three S. aureus strains, including methicillin-resistant S. aureus and quinolone-resistant S. aureus (QRSA), DW286 demonstrated the most potent activity, as found in vitro. Specially, DW286 is ≥8-fold more active against QRSA than the other fluoroquinolones. And the 50% protective doses for DW286 were correspondent with the in vitro activities.

Sign in / Sign up

Export Citation Format

Share Document