scholarly journals Synthesis, Anti-Bacterial and Anti-biofilm Activity of New Iminothiazolidinones

2021 ◽  
pp. 33-40
Author(s):  
Kumaraswamy Gullapelli ◽  
Ravichander Maroju
Keyword(s):  
Methicillin Resistant Staphylococcus Aureus ◽  
Simple Procedure ◽  
Chloroacetic Acid ◽  
Bacterial Strains ◽  
Reaction Conditions ◽  
Biofilm Inhibition ◽  
Wide Range ◽  
Potential Activity ◽  
Vancomycin Resistant ◽  
Pharmaceutical Properties

Aim: Iminothiazolidinones are one of the important classes of heterocyclic compounds and they occupied unique position in medicinal chemistry due to their wide range of biological and pharmaceutical properties. In view this potential activity, it has been planned to synthesize a series of New Iminothiazolidinones on benzimidazole nucleus and to study their biological activity. Methodology: Iminothiazolidinones and 1,1 dioxide- Iminothiazolidinones were synthesized with a simple and efficient method of cyclic condensation of aryl thiourea containing benzimidazole and thiazole with chloroacetic acid .This method requires mild reaction conditions, simple procedure and gives good yield. Results: The structures of the synthesized compounds were assessed by Infrared, NMR and Mass spectroscopic methods. The synthesized compounds were screened for their antibacterial and biofilm inhibitory activities against selected multi drug resistant bacterial strains. Conclusion: In accordance with the results obtained, growth inhibition was found significant with compounds 5d and 5e. Methicillin resistant Staphylococcus aureus (MRSA), Vancomycin resistant Enterococcus (VRE), and extended spectrum β‑lactamase (ESBL) producing Klebsiella pneumoniae have shown varied susceptibility towards these compounds. The Biofilm inhibition Concentrations (BFIC) of compounds 5e and 5d are 3.22 ±0.56 and 6.58 ±1.5 µg/mL respectively were noted against MRSA.

scholarly journals Synthesis and characterization of β-carboline fatty alcohol hybrids as potential biological active and antioxidant molecules

2020 ◽  
Author(s):  
Venkateshwarlu Kontham ◽  
Bhavya Ippakayala ◽  
Devarapaga Madhu
Keyword(s):  
Fatty Alcohol ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Bacterial Strains ◽  
Anticancer Compounds ◽  
Biofilm Inhibition ◽  
Spectral Techniques ◽  
Ester Linkage ◽  
Potential Activity

Nine new β-carboline fatty alcohol hybrids were synthesized from natural amino acid L-tryptophan and hybridized with 10-undecenol via ester linkage. All the synthesized products were characterized in each step by spectral techniques (1H, 13C NMR mass and HRMS). Synthesized β-carboline derivatives (7a-i) were screened for biological activities such as antimicrobial, antifungal, antibio film and anticancer. Compounds 7d and 7f showed most potent antimicrobial activity against B.subtilis MTCC 121, M.luteus MTCC 2470, S.aureus MTCC 96 and C.albicans MTCC 3017 bacterial strains ranged from 2.8 to 28.3 µg/mL. Biofilm inhibition assay showed that the compound 7f exhibited better activity against three bacterial stains with IC50 values from 1.8 to 2.9 µM. All the β-carboline derivatives showed cytotoxic activity, among them compounds 7f and 7h (IC50 values 9.1 and 11.4 µM) were exhibited potential activity. Free radical scavenging activity via DPPH assay revealed that compound 7g acted as good antioxidant molecule than all the tested compounds.

scholarly journals Total Synthesis and Antimicrobial Evaluation of 23-Demethyleushearilide and Extensive Antimicrobial Evaluation of All Synthetic Stereoisomers of (16Z,20E)-Eushearilide and (16E,20E)-Eushearilide

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3437 ◽  
Author(s):  
Takayuki Tonoi ◽  
Takehiko Inohana ◽  
Teruyuki Sato ◽  
Yuuki Noda ◽  
Miyuki Ikeda ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Total Synthesis ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Fungal Infections ◽  
Lead Compounds ◽  
Structure Activity ◽  
Vancomycin Resistant Enterococci ◽  
Wide Range ◽  
Antimicrobial Evaluation ◽  
Vancomycin Resistant

A novel stereoisomer of eushearilide, 23-demethyleushearilide, was synthesized, and the structure–activity relationships of this compound along with known eushearilide stereoisomers were investigated in order to design novel lead compounds for the treatment of fungal infections. It was discovered that all of these congeners, together with the natural product, exhibited a wide range of antimicrobial activity against not only fungi but also against bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE).

scholarly journals Case Report of a Successful Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) Bacteremia and MRSA/Vancomycin-Resistant Enterococcus faecium Cholecystitis by Daptomycin

2011 ◽  
Vol 55 (5) ◽  
pp. 2458-2459 ◽  
Author(s):  
Carlo Tascini ◽  
Antonello Di Paolo ◽  
Marialuisa Polillo ◽  
Mauro Ferrari ◽  
Paola Lambelet ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Enterococcus Faecium ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Drug Dose ◽  
Vancomycin Resistant Enterococcus ◽  
Bacterial Strains ◽  
Methicillin Resistant ◽  
Content Type ◽  
Bile Concentration ◽  
Vancomycin Resistant

ABSTRACTA 72-year-old man, receiving 8 mg daptomycin/kg body weight/day for methicillin-resistantStaphylococcus aureus(MRSA) bacteremia, was diagnosed with MRSA/vancomycin-resistantEnterococcus faecium(VRE) cholecystitis (daptomycin MIC values, 1 and 2 mg/liter, respectively). After the fifth drug dose, the bile concentration of daptomycin was 66 mg/liter 5 min after drug administration, with the biliary concentration/MIC values higher than 30 for both bacterial strains. Therefore, daptomycin achieved therapeutic levels in bile, hence suggesting a role for the drug in the treatment of MRSA/VRE cholecystitis.

scholarly journals Bacteriophage Therapy Rescues Mice Bacteremic from a Clinical Isolate of Vancomycin-Resistant Enterococcus faecium

2002 ◽  
Vol 70 (1) ◽  
pp. 204-210 ◽  
Author(s):  
Biswajit Biswas ◽  
Sankar Adhya ◽  
Paul Washart ◽  
Brian Paul ◽  
Andrei N. Trostel ◽  
...  
Keyword(s):  
Enterococcus Faecium ◽  
The United States ◽  
Bacterial Strains ◽  
Bacteriophage Therapy ◽  
Functional Capabilities ◽  
Wide Range ◽  
Phage Strain ◽  
Vancomycin Resistant ◽  
The Individual

ABSTRACT Colonization of the gastrointestinal tract with vancomycin-resistant Enterococcus faecium (VRE) has become endemic in many hospitals and nursing homes in the United States. Such colonization predisposes the individual to VRE bacteremia and/or endocarditis, and immunocompromised patients are at particular risk for these conditions. The emergence of antibiotic-resistant bacterial strains requires the exploration of alternative antibacterial therapies, which led our group to study the ability of bacterial viruses (bacteriophages, or phages) to rescue mice with VRE bacteremia. The phage strain used in this study has lytic activity against a wide range of clinical isolates of VRE. One of these VRE strains was used to induce bacteremia in mice by intraperitoneal (i.p.) injection of 109 CFU. The resulting bacteremia was fatal within 48 h. A single i.p. injection of 3 × 108 PFU of the phage strain, administered 45 min after the bacterial challenge, was sufficient to rescue 100% of the animals. Even when treatment was delayed to the point where all animals were moribund, approximately 50% of them were rescued by a single injection of this phage preparation. The ability of this phage to rescue bacteremic mice was demonstrated to be due to the functional capabilities of the phage and not to a nonspecific immune effect. The rescue of bacteremic mice could be effected only by phage strains able to grow in vitro on the bacterial host used to infect the animals, and when such strains are heat inactivated they lose their ability to rescue the infected mice.

scholarly journals Lipoteichoic Acid Biosynthesis Inhibitors as Potent Inhibitors of S. aureus and E. faecalis Growth and Biofilm Formation

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2277
Author(s):  
George A. Naclerio ◽  
Kenneth I. Onyedibe ◽  
Herman O. Sintim
Keyword(s):  
Biofilm Formation ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Lipoteichoic Acid ◽  
Acid Biosynthesis ◽  
Biofilm Inhibition ◽  
Teichoic Acids ◽  
Biosynthesis Inhibitors ◽  
New Chemical Entities ◽  
Vancomycin Resistant ◽  
Wall Teichoic Acids

Methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VRE) have been deemed as serious threats by the CDC. Many chronic MRSA and VRE infections are due to biofilm formation. Biofilm are considered to be between 10–10,000 times more resistant to antibiotics, and therefore new chemical entities that inhibit and/or eradicate biofilm formation are needed. Teichoic acids, such as lipoteichoic acids (LTAs) and wall teichoic acids (WTAs), play pivotal roles in Gram-positive bacteria’s ability to grow, replicate, and form biofilms, making the inhibition of these teichoic acids a promising approach to fight infections by biofilm forming bacteria. Here, we describe the potent biofilm inhibition activity against MRSA and VRE biofilms by two LTA biosynthesis inhibitors HSGN-94 and HSGN-189 with MBICs as low as 0.0625 µg/mL against MRSA biofilms and 0.5 µg/mL against VRE biofilms. Additionally, both HSGN-94 and HSGN-189 were shown to potently synergize with the WTA inhibitor Tunicamycin in inhibiting MRSA and VRE biofilm formation.

Microwave-accelerated Approaches to Diverse Xanthenes: A Review

2020 ◽  
Vol 7 (2) ◽  
pp. 99-111
Author(s):  
Jagmeet Singh ◽  
Ankit Lathwal ◽  
Shalini Agarwal ◽  
Mahendra Nath
Keyword(s):  
Reaction Rates ◽  
Waste Generation ◽  
Reaction Conditions ◽  
Catalytic Systems ◽  
Heterocyclic Molecules ◽  
The Past ◽  
Wide Range ◽  
Pharmaceutical Properties ◽  
Synthetic Methodologies ◽  
High Yields

Microwave-accelerated methods have emerged as powerful tools in organic synthesis to enhance the reaction rates and provide products with high yields, improved selectivity, lower energy consumption, mild reaction conditions and negligible waste generation. Xanthenes are an important class of biologically important oxygen-containing heterocyclic molecules that possess a multitude of pharmaceutical properties. By considering the medicinal and material significance of these molecules, a large number of synthetic methodologies and catalytic systems have been reported for the synthesis of a wide range of xanthenes in the past. However, the focus of the present review is to summarize various microwave-assisted protocols for the synthesis of diversely substituted xanthene analogues.

Green synthesis and antibiofilm potential of Silver Nanoparticles loaded with Narcissus tazetta L. Extract

2021 ◽  
Vol 20 (2) ◽  
pp. 203-218
Author(s):  
Isra Ikram ◽  
Barkatullah ◽  
Shah Khalid ◽  
Hoor Shumail ◽  
Haroon Khan ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Aspergillus Terreus ◽  
Bacterial Strains ◽  
Narcissus Tazetta ◽  
Biofilm Inhibition ◽  
E Coli ◽  
Wide Range ◽  
Microbial Potential ◽  
Effective Drugs ◽  
Dose Dependent

Bacterial infections are the leading cause of mortality, due to the paucity of effective drugs. This study aimed to synthesize AgNPs loaded with fresh leaves & bulbs extracts of Narcissus tazetta and evaluate antimicrobial and antibiofilm potential against selected bacterial and fungal isolates using standard microbiological protocols. Different techniques like FTIR spectroscopy, GC-MS, electron microscopy and HPLC were used to characterize the AgNPs. The AgNPs synthesized from crude extract of leaves and bulb were checked and were found effective against all the bacterial isolates except E. coli however, strong biofilm inhibition potential was observed in case of E.coli. The synthesized AgNPs showed dose dependent zone of inhibition higher for methanol and lower for n-Hexane against both Gram + ve and Gram -ve bacterial strains, exhibiting the anti-microbial potential. Biofilm inhibition was recorded at sub-MIC values against Gram + ve and Gram -ve bacterial strains. Antifungal activity of AgNPs was observed only at a higher concentration against Aspergillus niger, Fusarium oxysporum and Alternaria alternata while Aspergillus terreus was resistant even at higher concentrations. In conclusion, we can say that the plant possesses pronounced antimicrobial potential with a wide range of the bioactive compounds, which can be explored for pharmaceutical purposes.

p-Sulfonic acid calix[n]arene catalyzed synthesis of bioactive heterocycles: A review

2020 ◽  
Vol 24 ◽  
Author(s):  
Bubun Banerjee ◽  
Gurpreet Kaur ◽  
Navdeep Kaur
Keyword(s):  
Supramolecular Chemistry ◽  
Sulfonic Acid ◽  
Catalytic Efficiency ◽  
The Other ◽  
Reaction Conditions ◽  
Metal Free ◽  
Bioactive Scaffolds ◽  
Wide Range ◽  
Efficient Alternative ◽  
Bioactive Heterocycles

: Metal-free organocatalysts are becoming an important tool for the sustainable developments of various bioactive heterocycles. On the other hand, during last two decades, calix[n]arenes have been gaining considerable attention due to their wide range of applicability in the field of supramolecular chemistry. Recently, sulfonic acid functionalized calix[n] arenes are being employed as an efficient alternative catalyst for the synthesis of various bioactive scaffolds. In this review we have summarized the catalytic efficiency of p-sulfonic acid calix[n]arenes for the synthesis of diverse biologically promising scaffolds under various reaction conditions. There is no such review available in the literature showing the catalytic applicability of p-sulfonic acid calix[n]arenes. Therefore, we strongly believe that this review will surely attract those researchers who are interested about this fascinating organocatalyst.

Sign in / Sign up

Export Citation Format

Share Document