scholarly journals Design, Synthesis and Biological Evaluation of New Piperazin-4-yl-(acetyl-thiazolidine-2,4-dione) Norfloxacin Analogues as Antimicrobial Agents

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3959 ◽  
Author(s):  
Marc ◽  
Araniciu ◽  
Oniga ◽  
Vlase ◽  
Pîrnău ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Binding Mode ◽  
Biological Properties ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Parent Molecule ◽  
Synthesis And Biological Evaluation

 In an effort to improve the antimicrobial activity of norfloxacin, a series of hybrid norfloxacin–thiazolidinedione molecules were synthesized and screened for their direct antimicrobial activity and their anti-biofilm properties. The new hybrids were intended to have a new binding mode to DNA gyrase, that will allow for a more potent antibacterial effect, and for activity against current quinolone-resistant bacterial strains. Moreover, the thiazolidinedione moiety aimed to include additional anti-pathogenicity by preventing biofilm formation. The resulting compounds showed promising direct activity against Gram-negative strains, and anti-biofilm activity against Gram-positive strains. Docking studies and ADMET were also used in order to explain the biological properties and revealed some potential advantages over the parent molecule norfloxacin.

scholarly journals Synthesis and biological evaluation of some new 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as antimicrobial agents

2022 ◽  
Vol 11 (1) ◽  
pp. 75-82 ◽  
Author(s):  
Iryna Myrko ◽  
Taras Chaban ◽  
Vasyl Matiychuk
Keyword(s):  
Mass Spectrometry ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Synthesis And Biological Evaluation

A series of some new pyrazole-substituted 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines was synthesized in this study. The structures of target substances were confirmed by using 1H and 13С NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds have been evaluated for antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial screening studies of synthesized substances established that 2 of 12 compounds show pronounced antibacterial activity against the strain Staphylococcus aureus.

New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation

2018 ◽  
Vol 18 (1) ◽  
pp. 75-87 ◽  
Author(s):  
Michelyne Haroun ◽  
Christophe Tratrat ◽  
Katerina Kositzi ◽  
Evangelia Tsolaki ◽  
Anthi Petrou ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Antimicrobial Properties ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Synthesis Methods ◽  
Design Synthesis ◽  
Benzothiazole Derivatives

Background: Thiazole and benzothiazole derivatives, as well as thiazolidinones are very important scaffolds in medicinal chemistry. Literature has revealed that they possess a wide spectrum of biological activities including antimicrobial activity. Objective: The goal of this paper is the designing of new benzothiazole based thiazolidinones and the evaluation of their biological activities. Methods: The designed compounds were synthesized using classical organic synthesis methods. The antimicrobial activity was evaluated using the method of microdilution. Results: The twelve newly synthesized compounds showed antimicrobial properties. All compounds appeared to be more active than ampicillin in most studied strains and in some cases, more active than streptomycin. Antifungal activity, in most cases was also better than the reference drugs ketoconazole and bifonazole. The prediction of cytotoxicity revealed that the synthesized compounds were not toxic (LD50 350-1000 mg/kg of body weight). Docking studies on the antibacterial activity confirmed the biological results. Conclusion: The twelve new compounds were synthesized and studied for their antimicrobial activity. The compounds appeared to be promising antimicrobial agents and could be the lead compounds for new, more potent drugs. According to the docking prediction, the compounds could be MurB inhibitors.

Design, synthesis and biological evaluation of novel 1,2,4-triazolo and 1,2,4-triazino[4,3-a]quinoxalines as potential anticancer and antimicrobial agents

MedChemComm ◽  
2015 ◽  
Vol 6 (1) ◽  
pp. 202-211 ◽  
Author(s):  
Doaa A. E. Issa ◽  
Nargues S. Habib ◽  
Abeer E. Abdel Wahab
Keyword(s):  
Antimicrobial Activity ◽  
Broad Spectrum ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Compound 9a showed dual anticancer and antimicrobial activity and compound 16 showed a broad spectrum antimicrobial activity.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

scholarly journals Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

2019 ◽  
pp. 300-307
Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
Anti Inflammatory ◽  
Physicochemical Data ◽  
Synthesis And Biological Evaluation

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF SPIRO (INDOLE-THIAZOLIDINE) DERIVATIVES AS ANTIMICROBIAL AGENTS

2019 ◽  
pp. 71-74
Author(s):  
PRIYANKA NIVRUTTI SHINDE ◽  
MANISH ASHOK RASKAR
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Aromatic Aldehydes ◽  
Catalytic Amount ◽  
Biological Evaluation ◽  
Mercaptoacetic Acid ◽  
Ir Absorption ◽  
Absorption Bands ◽  
Synthesis And Biological Evaluation ◽  
Anhydrous Zncl2

Objective: The present study aims to synthesize and biological evaluation of Spiro-[Indole-Thiazolidine] derivatives as antimicrobial agents. Methods: The reaction sequence involves microwave-induced preparation of N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene)pyridine-4-carbohydrazide [3] from isoniazid [1] and isatin [2] followed by the cyclo condensation of [3] and mercaptoacetic acid under microwave condition to achieve the synthesis of spiro-[indole-thiazolidine] derivatives [4]. The resulting compounds were then allowed to react with various aromatic and heterocyclic aromatic aldehydes to afford arylidene derivatives [5a-l]. Result: Isoniazid (1) on condensation with isatin (2) in the presence of catalytic amount of glacial acetic acid furnished N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene) pyridine-4-carbohydrazide (3), which showed characteristic IR, absorption bands. Compound (3) underwent Spiro cyclization upon its reaction with mercaptoacetic acid in the presence of anhydrous ZnCl2 to form spiro-[indole-thiazolidine] compound (4). Compound (4) was then condensed with aromatic aldehydes to give arylidene derivatives (5a-l), which were characterized by IR and 1H NMR spectral data. Conclusion: All the synthesized compounds were screened for antimicrobial activity by the cup plate method. Most of the derivatives showed good antimicrobial activity against Gram-Positive and Gram-negative bacteria.

scholarly journals Design, Synthesis and Biological Evaluation ofN-Sulfonylphenyl glyoxamide-Based Antimicrobial Peptide Mimics as Novel Antimicrobial Agents

2017 ◽  
Vol 2 (12) ◽  
pp. 3452-3461 ◽  
Author(s):  
Tsz Tin Yu ◽  
Shashidhar Nizalapur ◽  
Kitty K. K. Ho ◽  
Eugene Yee ◽  
Thomas Berry ◽  
...  
Keyword(s):  
Antimicrobial Peptide ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Peptide Mimics ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, Synthesis, and Biological Evaluation of Thieno[2,3-c]pyrazole Hydrazide Derivatives as Potential Antimicrobial Agents

2015 ◽  
Vol 54 (1) ◽  
pp. 44-50 ◽  
Author(s):  
Pravin S. Mahajan ◽  
Mukesh D. Nikam ◽  
Asha V. Chate ◽  
Anil S. Bobade ◽  
Charansingh H. Gill
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
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