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provides coniferyl ferulate(CAS#:91296-87-6) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
Background: Fluoroquinolones (FQs) are compounds of major interest with broad antimicrobial activities against community and hospital-acquired infections such as respiratory tract infections (nosocomial pneumonia, chronic bronchitis and tuberculosis), skin and soft tissue infections, bone and joint infections, intra-abdominal infections and sexually transmitted diseases. This broad range of activities along with favorable pharmacokinetic and low toxicity introduced this class of compounds as important antimicrobial chemotherapy agents. The rapid increase in prevalence of FQs resistant microbes in environment motivated medicinal chemists to discover new quinolone-based compounds with potent activities against Gram-positive bacteria.
Methods: The designed compounds were prepared through the two-component reaction between aromatic α-haloketones or α-halooximes and sarafloxacin in the presence of NaHCO3 in DMF, affording the corresponding N-[2-(aryl-3-yl) ethyl] piperazinyl quinolone derivatives in good yields. All synthesized compounds were evaluated for antibacterial activities against Gram-positive [Staphylococcus aureus ATCC 6538p, Micrococcus luteus, ATCC 1110, Staphylococcus epidermidis ATCC 12228 and Bacillus subtilis ATCC 6633] and Gram-negative [Escherichia coli ATCC 8739, Klebsiella pneumoniae ATCC 10031 Pseudomonas aeruginosa ATCC 9027 and Serratia marcescens PTCC 1111] bacteria.
Results: The antibacterial activities of 24 new compounds were reported as MIC values in comparison to sarafloxacin. The most active compound, 4 g, exhibited similar inhibitory activity against Gram-positive bacteria including S. aureus, S. epidermidis and B. subtilis compared to positive control. Furthermore, benzyloxime incorporated derivatives (4 s-4x) showed poor activity against all tested strains, except 4x.
Conclusion: The obtained results indicated that the synthesized compounds containing substituted piperazine moiety at the C-7 position displayed same or weak inhibitory activities compared to sarafloxacin. Graphical abstract
Antibacterial activity; Gram-positive bacteria; Quinolones; Synthesis.
N-substituted Piperazinyl Sarafloxacin Derivatives: Synthesis and in Vitro Antibacterial Evaluation
Ali Asadipour 1 2, Mohammad Hassan Moshafi 3, Leila Khosravani 4, Setareh Moghimi 4, Elham Amou 4, Loghman Firoozpour 4, Ghazaleh Ilbeigi 3, Keivan Beiki 3, Ehsan Soleimani 3, Alireza Foroumadi 5 6
In this study, the fluorescence spectra of sarafloxacin (SAR) under different pH conditions were investigated to determine the structural changes due to protonation that result from change in pH. At pH < 1.02, SAR exists in the H3 L2+ form for which the maximum fluorescence emission wavelength was about 455 nm. At pH 1.87-4.94, SAR exists in the H2 L+ form in which H3 L2+ loses one proton in the nitrogen molecule at the 1-position in the quinoline ring. Fluorescence intensity was strong and steady and the maximum emission wavelength was 458 nm. At pH 7.14-9.30, the maximum emission wavelengths were gradually blue shifted to 430 nm with increase in pH, here SAR exists in the form of a bipolar ion HL in which H2 L+ loses a carboxyl group proton. At pH > 11.6, HL transforms into anionic L- in which HL loses one proton from the piperazine ring, leading to a decrease in fluorescence intensity, and the maximum emission wavelength was red shifted to approximately 466 nm. The two-step dissociation constant pKa for SAR was calculated, pKa1 was 6.06 ± 0.37 and pKa2 for SAR was 10.53 ± 0.19. In a pH 3.62 buffer solution with quinine sulfate as the reference, the fluorescence quantum yield of SAR at the maximum excitation wavelength of 276 nm was 0.09.
dissociation constant; fluorescence quantum yield; fluorescence spectroscopy; sarafloxacin.
Fluorescence Spectra, Fluorescence Quantum Yield and Dissociation Constant of Sarafloxacin
Tongtong Li 1, Baosheng Liu 1, Shaotong Duan 1, Mengmeng Cui 1
The effect of sarafloxacin to Cu/ZnSOD was evaluated via investigating the change in Cu/ZnSOD structure and the structure basis activity upon sarafloxacin binding. Multi-spectroscopic methods, isothermal titration microcalorimetry (ITC) and molecular docking method were adopted in this study. Sarafloxacin binds to Cu/ZnSOD mainly through hydrophobic and hydrogen bond forces and tends to be saturated as the molar ratio of sarafloxacin to Cu/ZnSOD reaches 4. The binding changed the microenvironment around Tyr and the secondary structure of Cu/ZnSOD but did not affect the activity of Cu/ZnSOD. Molecular docking study revealed that sarafloxacin binds into a hydrophobic area with possibility to form hydrogen bonds with Tyr 108, Asp 25, Pro 100 and Ser 103 of Cu/ZnSOD. The binding area locates on the surface of β-barrel close to the second Greek key loop (GK2) and V-loop but far away from the active site and active site channel of Cu/ZnSOD. These promoted the understanding of the experiment phenomenons. The binding of sarafloxacin does not affect the activity of Cu/ZnSOD should attribute to the binding not to change the microenvironment of Cu/ZnSOD active site and active site channel.
Cu/ZnSOD; Enzyme activity; ITC; Molecular docking; Multi-spectroscopic methods; Sarafloxacin.
The Effect of Sarafloxacin on Cu/ZnSOD Structure and Activity
Zhaozhen Cao 1, Rutao Liu 2, Ziliang Dong 3, Xinping Yang 4, Yadong Chen 5
2015 Feb 5