ChemInform Abstract: Preparation and in vitro Antibacterial Activity of 9-O-Glycosyloxime Derivatives of Erythromycin A, a New Class of Macrolide Antibiotics

ChemInform ◽  
2010 ◽  
Vol 28 (13) ◽  
pp. no-no
Author(s):  
C. GRANDJEAN ◽  
G. LUKACS
Keyword(s):  
Antibacterial Activity ◽  
Macrolide Antibiotics ◽  
New Class ◽  
In Vitro Antibacterial Activity ◽  
Erythromycin A ◽  
Derivatives Of

Design, synthesis and antibacterial evaluation of ocotillol derivatives with polycyclic nitrogen-containing groups

2021 ◽  
Author(s):  
Yucheng Cao ◽  
Kaiyi Wang ◽  
Jiali Wang ◽  
Haoran Cheng ◽  
Mengxin Ma ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Multidrug Resistant ◽  
Inhibitory Effect ◽  
Resistant Bacteria ◽  
Design Synthesis ◽  
In Vitro Antibacterial Activity ◽  
Strong Inhibitory Effect ◽  
Hospital Acquired ◽  
Derivatives Of

Aim: With the increasing abuse of antibacterial drugs, multidrug-resistant bacteria have become a burden on human health and the healthcare system. To find alternative compounds effective against hospital-acquired methicillin-resistant Staphylococcus aureus (HA-MRSA), novel derivatives of ocotillol were synthesized. Methods & Results: Ocotillol derivatives with polycyclic nitrogen-containing groups were synthesized and evaluated for in vitro antibacterial activity. Compounds 36–39 exhibited potent antibacterial activity against hospital-acquired MRSA, with MIC = 8–64 μg/ml. Additionally, a combination of compound 37 and the commercially available antibiotic kanamycin showed synergistic inhibitory effects, with a fractional inhibitory concentration index of ≤0.375. Conclusion: Compound 37 has a strong inhibitory effect, and this derivative has potential for use as a pharmacological tool to explore antibacterial mechanisms.

scholarly journals Investigation of antibacterial activity of cinnamyl derivatives of arylpiperazine

2012 ◽  
Vol 64 (1) ◽  
pp. 15-20 ◽  
Author(s):  
Irena Novakovic ◽  
Jelena Penjisevic ◽  
V. Sukalovic ◽  
Deana Andric ◽  
G. Roglic ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Salmonella Enteritidis ◽  
Antibacterial Activities ◽  
Diffusion Method ◽  
Disc Diffusion ◽  
Disc Diffusion Method ◽  
Clostridium Sporogenes ◽  
In Vitro Antibacterial Activity ◽  
Derivatives Of

The derivatives of cinnamic acid and N-arylpiperazine show antibacterial activity. In this work the potential synergistic effect of cinnamyl derivatives of arylpiperazine in selected bacteria was investigated. The antibacterial activities of the derivatives were evaluated against Gram-positive bacteria: Staphylococcus aureus, Streptosporangium longisporum, Sarcina lutea, Micrococcus flavus, Clostridium sporogenes and Bacillus subtilis and Gram-negative bacteria: Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis and Proteus vulgaris by the disc diffusion method. The minimum inhibitory concentration (MIC) against the selected bacteria was determined for all compounds that showed activity in the disc diffusion method. The majority of the investigated compounds displayed in vitro antibacterial activity. The effect of the type and structure of the substituent on the aromatic ring on the antibacterial activity is discussed. It was found that two derivatives expressed activity toward S. longisporum and P. aeruginosa that was almost as strong as that of amikacin.

scholarly journals A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1776 ◽  
Author(s):  
Javier Campanini-Salinas ◽  
Juan Andrades-Lagos ◽  
Gerardo Gonzalez Rocha ◽  
Duane Choquesillo-Lazarte ◽  
Soledad Bollo Dragnic ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
New Class ◽  
Microdilution Method ◽  
Mammalian Cell Lines ◽  
Broth Microdilution Method ◽  
In Vitro Antibacterial Activity ◽  
In Vitro Data

A rapid emergence of resistant bacteria is occurring worldwide, endangering the efficacy of antibiotics and reducing the therapeutic arsenal available for treatment of infectious diseases. In the present study, we developed a new class of compounds with antibacterial activity obtained by a simple, two step synthesis and screened the products for in vitro antibacterial activity against ATCC® strains using the broth microdilution method. The compounds exhibited minimum inhibitory concentrations (MIC) of 1–32 μg/mL against Gram-positive ATCC® strains. The structure–activity relationship indicated that the thiophenol ring is essential for antibacterial activity and the substituents on the thiophenol ring module, for antibacterial activity. The most promising compounds detected by screening were tested against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VREF) clinical isolates. We found remarkable activity against VREF for compounds 7 and 16, were the MIC50/90 were 2/4 µg/mL and 4/4 µg/mL, respectively, while for vancomycin the MIC50/90 was 256/512 µg/mL. Neither compound affected cell viability in any of the mammalian cell lines at any of the concentrations tested. These in vitro data show that compounds 7 and 16 have an interesting potential to be developed as new antibacterial drugs against infections caused by VREF.

scholarly journals In vitro activities of new quinolones against Helicobacter pylori.

1997 ◽  
Vol 41 (12) ◽  
pp. 2790-2792 ◽  
Author(s):  
M Carbone ◽  
M T Fera ◽  
V Cecchetti ◽  
O Tabarrini ◽  
E Losi ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Antibacterial Activity ◽  
Fluorine Atom ◽  
New Class ◽  
New Quinolones ◽  
In Vitro Antibacterial Activity ◽  
Inhibitory Activities ◽  
H Pylori

Compounds belonging to a new class of quinolones in which the fundamental C-6 fluorine atom was replaced were evaluated for in vitro antibacterial activity against 32 Helicobacter pylori strains. Since these substitutions resulted in higher inhibitory activities, these new desfluoroquinolones may be useful in eradicating H. pylori infections.

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