scholarly journals SYNTHESIS, MOLECULAR DOCKING AND ANTIBACTERIAL EVALUATION OF SOME NOVEL N-4 PIPERIDINYL DERIVATIVES OF SPARFLOXACIN

2018 ◽  
Vol 11 (10) ◽  
pp. 415
Author(s):  
Hemanth K Sudheer Kumar ◽  
Parameshwar H
Keyword(s):  
Antibacterial Activity ◽  
Benzoyl Chloride ◽  
Docking Simulation ◽  
Binding Modes ◽  
Minimum Inhibitory Concentrations ◽  
Good Antibacterial Activity ◽  
Analysis Technique ◽  
1H Nuclear Magnetic Resonance ◽  
Derivatives Of

Objective: The present study envisage a series of sparfloxacin derivatives were synthesized (Q1-Q10) with added derivatives such as aminomethyl benzenesulfenyl, methyl (methylamino)benzenesulfenyl, amino methyl benzoyl chloride, nitromethyl benzoyl chloride, dimethyl phenylamino, methoxymethyl phenylamino, dimethyl oxopyrazol, methyl dioxopyrrolidine, methyl oxopyrrolidine, and N-Boc amino methyl methylpyrrolidine through N-Piperzinyl linkage.Methods: All the newly synthesized compounds were characterized by infrared,1H nuclear magnetic resonance, mass spectrometry, and elemental analysis technique, screened for docking stimulation to find out binding modes of synthesized derivatives with 3FV5 and 3IMW, and evaluated for in vitro antimicrobial activity.Results: From this study, it was found that the compound Q5 showed good antibacterial activity against Gram-positive (Staphylococcus aureus) and compound Q4 showed good antibacterial activity against Gram-negative (Escherichia coli) in comparison with standard drugs (ciprofloxacin and sparfloxacin). The zone of inhibition and minimum inhibitory concentrations studies performed to synthesized compounds. The correlation between experimental data (minimum inhibitory concentrations) and docking score suggests that penetration for docking simulation is good to mild in reproducing experimental orientation of these synthesized compounds.Conclusion: The analogs of sparfloxacin are suggested to be potent inhibitors with sufficient scope for further exploration.

scholarly journals SYNTHESIS, MOLECULAR BIOINFORMATICS MODELLING, AND ANTIMICROBIAL EVALUATION OF SOME NOVEL OXADIAZOLE FLUOROQUINOLONE DERIVATIVES

2021 ◽  
pp. 40-46
Author(s):  
NAWAZ MOHAMMED KHAN ◽  
PAWAN KUMAR ◽  
HEMANTH SUDHEER KUMAR K ◽  
BHARATH RATHNA KUMAR P
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Concentration ◽  
Binding Modes ◽  
Zone Of Inhibition ◽  
Good Antibacterial Activity ◽  
Analysis Technique ◽  
1H Nuclear Magnetic Resonance ◽  
Antimicrobial Evaluation ◽  
Fluoroquinolone Derivatives

Objective: The present study envisages a series of oxadiazole fluoroquinolone derivatives that were synthesized (D1–D12) with added derivatives such as phenyl, aminophenyl, amino hydroxyphenyl along with cyclopropyl, ethyl, piperazine, and imidazole. Methods: All of the newly produced molecules were characterized by infrared, 1H nuclear magnetic resonance, mass spectrometry, and elemental analysis technique and screened for docking stimulation to find out binding modes of synthesized derivatives with 3FV5, 5IMW, and 5ESE and evaluated for in vitro antimicrobial activity. Results: From this study, it was found that the compound D8 showed good antibacterial activity against Gram-positive (Staphylococcus aureus), compound D9 showed good antibacterial activity against Gram-negative (Escherichia coli), and compound D3 showed good antifungal activity against fungi (Saccharomyces cerevisiae) in comparison with standard drugs (Ciprofloxacin and fluconazole). The zone of inhibition and minimum inhibitory concentration studies was performed on synthesized compounds. Conclusion: The analogs of oxadiazole flouroquinolone are suggested to be potent inhibitors with sufficient scope for further exploration.

scholarly journals Synthesis, Characterization and Antibacterial Activity of Carbamate Derivatives of Isatin

2018 ◽  
Vol 34 (4) ◽  
pp. 2026-2030 ◽  
Author(s):  
Sarrah Sattar Jabbar
Keyword(s):  
Amino Acids ◽  
Antibacterial Activity ◽  
Antibacterial Agent ◽  
Antibacterial Properties ◽  
E Coli ◽  
Good Antibacterial Activity ◽  
Diffusion Technique ◽  
Derivatives Of ◽  
Isatin Derivatives

In search of novel antibacterial agent, a series of new isatin derivatives (3a-d) have been synthesized by condensation isatin (2,3-indolinendione) with piperidine (hexahydropyridine), hydrazine hydrate and Boc-amino acids respectively. Compounds synthesized have been characterized by IR spectroscopy and elemental analysis. In addition, the in vitro antibacterial properties have been tested against E. coli, P. aeruginosa, and Bacillus cereus, S. aureus by employing the well diffusion technique. A majority of the synthesized compounds were showing good antibacterial activity and from comparisons of the compounds, compound 3d has been determined to be the most active compound.

Synthesis and Evaluation of Aromatic Surfactants as Potential Antibacterial and Cytotoxic Agents

2019 ◽  
Vol 16 (6) ◽  
pp. 478-484
Author(s):  
Kenia Barrantes ◽  
Mary Fuentes ◽  
Luz Chacón ◽  
Rosario Achí ◽  
Jorge Granados-Zuñiga ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Hela Cells ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Hydroxybenzoic Acid ◽  
Derivatives Of

Two ether and one ester derivatives of the 4-nitro-3-hydroxybenzoic acid were synthesized and characterized. The in vitro antimicrobial and cytotoxic activities of the three novel compounds were also evaluated. The aromatic derivatives showed antibacterial activity against one of the four microorganisms tested and two compounds (C8 and NOBA) had a lower IC50 in HeLa cells.

Synthesis, Molecular Modelling and Antibacterial Activity Against Helicobacter pylori of Novel Diflunisal Derivatives as Urease Enzyme Inhibitors

2019 ◽  
Vol 16 (4) ◽  
pp. 392-400 ◽  
Author(s):  
Göknil Pelin Coşkun ◽  
Teodora Djikic ◽  
Sadık Kalaycı ◽  
Kemal Yelekçi ◽  
Fikrettin Şahin ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Antibacterial Activity ◽  
Enzyme Inhibitors ◽  
Binding Modes ◽  
Bacterial Strains ◽  
Urease Enzyme ◽  
H Pylori ◽  
Ulcer Treatment ◽  
Main Factor

Background:The main factor for the prolongation of the ulcer treatment in the gastrointestinal system would be Helicobacter pylori infection, which can possibly lead to gastrointestinal cancer. Triple therapy is the treatment of choice by today's standards. However, observed resistance among the bacterial strains can make the situation even worse. Therefore, there is a need to discover new targeted antibacterial therapy in order to make success in the eradication of H. pylori infections.Methods:The targeted therapy rule is to identify the related macromolecules that are responsible for the survival of the bacteria. Thus, 2-[(2',4'-difluoro-4-hydroxybiphenyl-3-yl)carbonyl]-N- (substituted)hydrazinocarbothioamide (3-13) and 5-(2',4'-difluoro-4-hydroxybiphenyl-3-yl)-4- (substituted)-2,4-dihydro-3H-1,2,4-triazole-3-thiones (14-17) were synthesized and evaluated for antibacterial activity in vitro against H. pylori.Results:All of the tested compounds showed remarkable antibacterial activity compared to the standard drugs (Ornidazole, Metronidazole, Nitrimidazin and Clarithromycin). Compounds 4 and 13 showed activity as 2µg/ml MIC value.Conclusion:In addition, we have investigated binding modes and energy of the compounds 4 and 13 on urease enzyme active by using the molecular docking tools.

scholarly journals SYNTHESIS AND ANTIMICROBIAL EVALUATION OF QUINAZOLINONE PEPTIDE DERIVATIVES

2017 ◽  
Vol 10 (16) ◽  
pp. 7 ◽  
Author(s):  
Bhupinder Kapoor ◽  
Arshid Nabi ◽  
Reena Gupta ◽  
Mukta Gupta
Keyword(s):  
Antibacterial Activity ◽  
Amino Acid ◽  
Antimicrobial Agents ◽  
Methyl Esters ◽  
Standard Drug ◽  
Amino Acid Peptide ◽  
Chemical Structures ◽  
1H Nuclear Magnetic Resonance ◽  
Peptide Derivatives ◽  
Derivatives Of

  Objective: The increased microbial resistance against commercially available drugs initiated the development of novel and safe antimicrobial agents in last few decades. In this view, a series of amino acid/dipeptide derivatives of quinazolin-3(4H)-one was synthesized and was evaluated for their antimicrobial potential.Method: Synthesis of amino acid/peptide derivatives were carried out by coupling 5-(2-(2-chlorophenyl)-4-oxoquinazolin-3(4H)-yl)-2-hydroxy benzoic acid with amino acid/dipeptide methyl esters in the presence of dicyclohexylcarbodiimide and N-methylmorpholine. The chemical structures of synthesized compounds were characterized by 1H nuclear magnetic resonance and infrared spectroscopy and were screened for antibacterial activity by disc diffusion method.Results: All the synthesized derivatives exhibited moderate to significant antibacterial activity against both Gram-positive and Gram-negative bacteria. The potency of compound 5d was comparable to standard drug ciprofloxacin in all the strains of bacteria used. The compound 5a was found to be more active against Streptococcus pyogenes and Staphylococcus aureus while compound 5c against Pseudomonas aeruginosa and Escherichia coli. Conclusion: Peptide derivatives of quinazolinone are promising antimicrobial agent and can be used for the synthesis of other novel compounds.

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 Derivatives of the β-Crinane Amaryllidaceae Alkaloid Haemanthamine as Multi-Target Directed Ligands for Alzheimer’s Disease

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1307 ◽  
Author(s):  
Eliška Kohelová ◽  
Rozálie Peřinová ◽  
Negar Maafi ◽  
Jan Korábečný ◽  
Daniela Hulcová ◽  
...  
Keyword(s):  
Active Sites ◽  
Glycogen Synthase ◽  
Binding Modes ◽  
Structural Determinants ◽  
Inhibitory Potential ◽  
Gsk 3Β ◽  
Inhibition Potency ◽  
Derivatives Of ◽  
In Vitro Data

Twelve derivatives 1a–1m of the β-crinane-type alkaloid haemanthamine were developed. All the semisynthetic derivatives were studied for their inhibitory potential against both acetylcholinesterase and butyrylcholinesterase. In addition, glycogen synthase kinase 3β (GSK-3β) inhibition potency was evaluated in the active derivatives. In order to reveal the availability of the drugs to the CNS, we elucidated the potential of selected derivatives to penetrate through the blood-brain barrier (BBB). Two compounds, namely 11-O-(2-methylbenzoyl)-haemanthamine (1j) and 11-O-(4-nitrobenzoyl)-haemanthamine (1m), revealed the most intriguing profile, both being acetylcholinesterase (hAChE) inhibitors on a micromolar scale, with GSK-3β inhibition properties, and predicted permeation through the BBB. In vitro data were further corroborated by detailed inspection of the compounds’ plausible binding modes in the active sites of hAChE and hBuChE, which led us to provide the structural determinants responsible for the activity towards these enzymes.

scholarly journals Microwave Induced Synthesis and Antimicrobial Activities of Some Derivatives of 3, 5-Diaryl-2-pyrazoline-1-carbaldehyde

2010 ◽  
Vol 7 (2) ◽  
pp. 496-500 ◽  
Author(s):  
Ravindra Kumar ◽  
Y. K. Srivastava
Keyword(s):  
Antibacterial Activity ◽  
Hydrazine Hydrate ◽  
Antimicrobial Activities ◽  
Derivatives Of ◽  
Phenylene Diamine

3, 5-Diaryl-2-pyrazoline-1-carbaldehyde(1)was condensed with hydrazine hydrate ando-phenylene diamine to afford corresponding hydrazones(2)and 3-benzimidazolyl-3, 5-diaryl-2-pyrazoline respectively under MWI condition. The newly synthesized compounds have been screened for their antibacterial activityin vitro.

Synthesis and in vitro antibacterial activity of novel fluoroalkyl-substituted pyrazolyl oxazolidinones

RSC Advances ◽  
2015 ◽  
Vol 5 (90) ◽  
pp. 73660-73669 ◽  
Author(s):  
Lili Yan ◽  
Jingjing Wu ◽  
Heng Chen ◽  
Shaowu Zhang ◽  
Zhi Wang ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Bacterial Pathogens ◽  
Gram Positive ◽  
Good Antibacterial Activity ◽  
In Vitro Antibacterial Activity

A series of novel fluoroalkyl-substituted pyrazole bearing oxazolidinone derivatives were synthesized and evaluated for their antibacterial activity against six Gram-positive bacterial pathogens. Most have good antibacterial activity, three being comparable to linezolid.

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