Synthesis and Antibacterial Activity of Thioureido Amide of Fluoroquinolone

Patel, Navin B.; Patel, Sarvil D.; Patel, Jignesh N; Patel, Jaymin C.; Gorgamwala, Y.S.

doi:10.3923/ijbc.2011.37.45

Cited by 8 publications

(4 citation statements)

References 9 publications

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“…FFE results in a differential deflection of charged sample components as they move toward the collection outlets. This allows the high-throughput separation of samples, such as low-molecular-weight organic compounds, 1 peptides, proteins, protein complexes,2 membranes,3 organelles,4 and whole cells 5. Isoelectric focusing (IEF), one of the modes that FFE supports, is a technique that separates and concentrates proteins based upon their isoelectric point (pI).…”

Section: Introductionmentioning

confidence: 99%

Microfluidic Preparative Free-Flow Isoelectric Focusing: System Optimization for Protein Complex Separation

et al. 2010

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Isoelectric Focusing (IEF) is the first step for two-dimensional (2D) gel electrophoresis and plays an important role in sample purification for proteomics. However, biases in protein size and pI resolution, as well as limitations in sample volume, gel capacity, sample loss, and experimental time, remain challenges. In order to address some of the limitations of traditional IEF, we present a microfluidic free flow IEF (FF-IEF) device for continuous protein separation into 24 fractions. The device reproducibly establishes a nearly linear pH gradient from 4 to 10. Optimized dynamic coatings of 4% poly (vinyl) alcohol (PVA) minimize peak broadening by transverse electrokinetic flows. Even though the device operates at high electric fields (up to 370V/cm) efficient cooling maintains solution temperature inside the separation channel controllably in the range 2 -25 °C. Protein samples with a dynamic concentration range between µg/mL to mg/mL can be loaded into the micro device at a flow rate of 1 mL/hr and residence time of ~12 min. By using a protein complex of 9 proteins and 13 isoforms, we demonstrate improved separation with the FF-IEF system over traditional 2D gel electrophoresis. Device to device reproducibility is also illustrated through the efficient depletion of the albumin and hemoglobin assays. Post-device sample concentrations result in a 10 to 20-fold increase, which allow for isolation and detection of low abundance proteins. The separation of specific proteins from a whole cell lysate is demonstrated as an example. The micro device has the further benefits of retaining high molecular weight proteins, providing higher yield of protein that has a broader range in pI, and reducing experimental time compared to conventional IEF IGP gel strip approaches.

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Section: Introductionmentioning

confidence: 99%

Microfluidic Preparative Free-Flow Isoelectric Focusing: System Optimization for Protein Complex Separation

et al. 2010

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“…29 Since the 1980s, uoroquinolones have been employed in pharmaceutical processes and the treatment of diverse bacterial infections. 30 The synthesis of quinoline and its derivatives can be performed using different methods due to the increasing interest in them. This is because of their array of documented applications in pharmaceutical processes.…”

Section: Historical Background Of Quinolinementioning

confidence: 99%

Recent advances in chemistry and therapeutic potential of functionalized quinoline motifs – a review

2022

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“…The thiourea skeleton favors other chemical modulations (e.g., incorporation of fluorine), these derivatives being thus promising candidates, both as active molecules and ligands. For instance, the fluoroquinolone derivatives having thioureido moiety and piperazin-1-yl groups have shown a significant improvement of the activity against Gram-positive (S. aureus, B. subtilis) and Gram-negative (E. coli, P. aeruginosa) bacterial strains [32]. The 2-(6'-fluorobenzothiazol-2'-ylamino)-4,6-(disubstituted thioureido)-1,3-pyrimidine derivatives and the 1-(isomeric fluorobenzoyl)-3-(isomeric fluorophenyl)thiourea compounds have shown inhibitory activity against the above-mentioned four species, correlated with the presence of nitro groups and with the presence and position of fluorine substituent on aroyl and aryl rings [33,34].…”

Section: Introductionmentioning

confidence: 99%

New Substituted Benzoylthiourea Derivatives: From Design to Antimicrobial Applications

et al. 2020

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The increasing threat of antimicrobial resistance to all currently available therapeutic agents has urged the development of novel antimicrobials. In this context, a series of new benzoylthiourea derivatives substituted with one or more fluorine atoms and with the trifluoromethyl group have been tested, synthesized, and characterized by IR, NMR, CHNS and crystal X-ray diffraction. The molecular docking has provided information regarding the binding affinity and the orientation of the new compounds to Escherichia coli DNA gyrase B. The docking score predicted the antimicrobial activity of the studied compounds, especially against E. coli, which was further demonstrated experimentally against planktonic and biofilm embedded bacterial and fungal cells. The compounds bearing one fluorine atom on the phenyl ring have shown the best antibacterial effect, while those with three fluorine atoms exhibited the most intensive antifungal activity. All tested compounds exhibited antibiofilm activity, correlated with the trifluoromethyl substituent, most favorable in para position.

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Synthesis and Antibacterial Activity of Thioureido Amide of Fluoroquinolone

Cited by 8 publications

References 9 publications

Microfluidic Preparative Free-Flow Isoelectric Focusing: System Optimization for Protein Complex Separation

Microfluidic Preparative Free-Flow Isoelectric Focusing: System Optimization for Protein Complex Separation

Recent advances in chemistry and therapeutic potential of functionalized quinoline motifs – a review

New Substituted Benzoylthiourea Derivatives: From Design to Antimicrobial Applications

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