Synthesis and in vitro Antibacterial Activity of Novel Heterocyclic Derivatives of 18-nor-Equilenin.

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.

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

ChemInform ◽

10.1002/chin.199713201 ◽

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

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Investigation of antibacterial activity of cinnamyl derivatives of arylpiperazine

Archives of Biological Sciences ◽

10.2298/abs1201015n ◽

2012 ◽

Vol 64 (1) ◽

pp. 15-20 ◽

Cited By ~ 2

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.

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