Identification, synthesis and biological activity of alkyl-guanidine oligomers as potent antibacterial agents

In an attempt to discover the new antibacterial agents to fight the bacterial infections, a series of 1,8-naphthyridine based 2-iminothiazolidin-4-one derivatives was synthesized by a straight-forward regioselective synthesis. 2-Phenyl-1,8-naphthyridin-3-amine (2) was reacted with acetyl or aroyl isothiocyantes to give the corresponding N-[(2-phenyl-1,8-naphthyridin-3-yl)carbamothioyl)]acetamide or benzamides (3a-e). Finally, the target compounds [N-(4-oxo-3-(2-phenyl-1,8-naphthyridin-3-yl)thiazolidin-2-ylidene)]acetamide or benzamides (4a-e) were obtained by the reaction of thiourea (3a-e) with chloroacetyl chloride in presence of pyridine. All the synthesized products were formed in good yields and their structures were characterized by spectral (IR, EI-MS and NMR) and physical data. The biological activity of title compounds was evaluated against the bacterial strains and found to be more potent.

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ChemInform Abstract: Hongoquercins, New Antibacterial Agents from the Fungus LL-23G227: Fermentation and Biological Activity.

ChemInform ◽

10.1002/chin.199905160 ◽

2010 ◽

Vol 30 (5) ◽

pp. no-no

Author(s):

D. A. ABBANAT ◽

M. P. SINGH ◽

M. GREENSTEIN

Keyword(s):

Biological Activity ◽

Antibacterial Agents

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Synthesis and biological activity of benzothiazolo[3,2-a]quinolone antibacterial agents

Journal of Medicinal Chemistry ◽

10.1021/jm00158a037 ◽

1986 ◽

Vol 29 (8) ◽

pp. 1531-1534 ◽

Cited By ~ 42

Author(s):

Daniel T. W. Chu ◽

Prabhavathi B. Fernandes ◽

Andre G. Pernet

Keyword(s):

Biological Activity ◽

Antibacterial Agents

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The Search for New Antibacterial Agents among 1,2,3-Triazole Functionalized Ciprofloxacin and Norfloxacin Hybrids: Synthesis, Docking Studies, and Biological Activity Evaluation

Scientia Pharmaceutica ◽

10.3390/scipharm90010002 ◽

2021 ◽

Vol 90 (1) ◽

pp. 2

Author(s):

Halyna Hryhoriv ◽

Illia Mariutsa ◽

Sergiy M. Kovalenko ◽

Victoriya Georgiyants ◽

Lina Perekhoda ◽

...

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Biological Activity ◽

Antibacterial Agents ◽

Docking Studies ◽

Synthetic Method ◽

Bacillus Subtilis Atcc ◽

Resistant Strains ◽

Derivatives Of

Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin and applying docking studies and biological activity evaluations in order to find active promising molecules. We succeeded in the development of a synthetic method towards 1,2,3-triazole-substituted ciprofloxacin and norfloxacin derivatives. The structure and purity of the obtained compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, LC/MS, UV-, IR- spectroscopy. Docking studies, together with in vitro research against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 27853, Candida albicans NCTC 885-653 revealed compounds in which activity exceeded the initial molecules.

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Effect of plant extract against opportunist human pathogen soil bacteria

Acta Agraria Debreceniensis ◽

10.34101/actaagrar/46/2415 ◽

2012 ◽

pp. 89-93

Author(s):

Csaba Tamás Tóth ◽

Mária Csubák

Keyword(s):

Public Health ◽

Biological Activity ◽

Soil Bacteria ◽

Laboratory Tests ◽

Pathogenic Bacteria ◽

Antibacterial Agents ◽

Ambrosia Artemisiifolia ◽

Biologically Active ◽

Human Pathogen ◽

Active Components

Our experiments have repeatedly shown that the extract of ragweed (Ambrosia artemisiifolia) is an antifungal and antibacterial component.In our paper we tested of the biological activity of the herbal substance against opportunistic human pathogenic bacteria strains (Staphylococcusaureus 110003 and 25923; Staphylococcus saprophyticus 110008). Our laboratory tests show that the extract is bacteriostatic and in several cases bactericid. We can assume that from the the agricultural and public health aspects can be extremely dangerous weed, contains biologically active components and it may be suitable for the prepare of antibacterial agents.

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Investigation of 5’-Norcarbocyclic Nucleoside Analogues as Antiprotozoal and Antibacterial Agents

Molecules ◽

10.3390/molecules24193433 ◽

2019 ◽

Vol 24 (19) ◽

pp. 3433 ◽

Cited By ~ 3

Author(s):

Anastasia Khandazhinskaya ◽

Elena Matyugina ◽

Pavel Solyev ◽

Maggie Wilkinson ◽

Karen Buckheit ◽

...

Keyword(s):

Mycobacterium Tuberculosis ◽

Biological Activity ◽

Antibacterial Agents ◽

Structure Activity Relationship ◽

Nucleoside Analogues ◽

Activity Relationship ◽

Carbocyclic Nucleosides ◽

Structure Activity ◽

Small Structure ◽

Relationship Study

Carbocyclic nucleosides have long played a role in antiviral, antiparasitic, and antibacterial therapies. Recent results from our laboratories from two structurally related scaffolds have shown promising activity against both Mycobacterium tuberculosis and several parasitic strains. As a result, a small structure activity relationship study was designed to further probe their activity and potential. Their synthesis and the results of the subsequent biological activity are reported herein.

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