scholarly journals Lipophilicity Determination of Quaternary (Fluoro)Quinolones by Chromatographic and Theoretical Approaches

2019 ◽  
Vol 20 (21) ◽  
pp. 5288 ◽  
Author(s):  
Krzesimir Ciura ◽  
Joanna Fedorowicz ◽  
Filip Andrić ◽  
Katarzyna Ewa Greber ◽  
Alina Gurgielewicz ◽  
...  
Keyword(s):  
Antimicrobial Activities ◽  
Reversed Phase ◽  
Theoretical Approaches ◽  
Sum Of Ranking Differences ◽  
Study Evaluation ◽  
Pharmacokinetic Properties ◽  
Software Platforms ◽  
Layer Chromatography ◽  
Lipophilic Character

Lipophilicity is a vital physicochemical parameter of a molecule, which affects several biological processes such as absorption, tissue distribution, and pharmacokinetic properties. In this study, evaluation of lipophilicities of a series of novel fluoroquinolone-Safirinium dye hybrids using chromatographic and computational methods is presented. Fluoroquinolone-Safirinium dye hybrids have been synthesized as new dual-acting hydrophilic antibacterial agents. Reversed phase thin-layer chromatography and micellar electrokinetic chromatography experiments were carried out. Furthermore, logP values of the target structures were predicted by means of different software platforms and algorithms. In order to assess similarities and dissimilarities of the obtained lipophilicity indexes, cluster analysis and sum of ranking differences were performed. The significant differences of calculated logP values (α = 0.05, p < 0.001) indicated that an experimental approach is necessary for lipophilicity prediction of this class of antibiotics. Chromatographic data indicated that the newly synthesized hybrid (fluoro)quinolone-based quaternary ammonium derivatives show less lipophilic character than the parent (fluoro)quinolones. Additionally, the chromatographically obtained lipophilicity indexes were evaluated for possible application in quantitative retention–activity relationships. The established lipophilicity models have the potential to predict antimicrobial activities of a series of quaternary (fluoro)quinolones against Bacillus subtilis, Escherichia coli, and Proteus vulgaris.

scholarly journals Synthesis, antimicrobial activity, and determination of the lipophilicity of ((cyclohex-3-enylmethylene)hydrazinyl)thiazole derivatives

2019 ◽  
Vol 28 (11) ◽  
pp. 2023-2036 ◽  
Author(s):  
Anna Biernasiuk ◽  
Magdalena Kawczyńska ◽  
Anna Berecka-Rycerz ◽  
Beata Rosada ◽  
Anna Gumieniczek ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Positive Control ◽  
Reversed Phase ◽  
Thiazole Derivatives ◽  
Strong Activity ◽  
Cytotoxicity Studies ◽  
L929 Fibroblast ◽  
Layer Chromatography

Abstract Synthesis and investigation of antimicrobial activity of fifteen novel thiazoles containing cyclohexene moiety are presented. Among the derivatives, compounds 3a–3d, 3f, 3n, and 3o showed very strong activity against the reference Candida spp. strains with MIC = 0.015–3.91 µg/ml. The activity of these compounds is similar and even higher than the activity of nystatin used as positive control. Compounds 3d, 3f, 3n, 3o showed the highest activity with very strong effect towards most of yeasts isolated from clinical materials with MIC = 0.015–7.81 µg/ml. The cytotoxicity studies for the most active compounds showed that Candida spp. growth was inhibited at noncytotoxic concentrations for the mammalian L929 fibroblast. In addition, a good correlation was obtained between lipophilicity of compounds determined using reversed phase thin-layer chromatography and their antifungal activity.

Determination of lipophilicity by means of reversed-phase thin-layer chromatography

1994 ◽  
Vol 669 (1-2) ◽  
pp. 246-253 ◽  
Author(s):  
G.L. Biagi ◽  
A.M. Barbaro ◽  
A. Sapone ◽  
M. Recanatini
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Reversed Phase ◽  
Layer Chromatography

scholarly journals Rapid, Highly-Sensitive and Ecologically Greener Reversed-Phase/Normal-Phase HPTLC Technique with Univariate Calibration for the Determination of Trans-Resveratrol

Separations ◽  
2021 ◽  
Vol 8 (10) ◽  
pp. 184
Author(s):  
Prawez Alam ◽  
Faiyaz Shakeel ◽  
Mohammed H. Alqarni ◽  
Ahmed I. Foudah ◽  
Mohammed M. Ghoneim ◽  
...  
Keyword(s):  
Mobile Phase ◽  
High Performance ◽  
Reversed Phase ◽  
Normal Phase ◽  
Commercial Formulation ◽  
Highly Sensitive ◽  
Validation Parameters ◽  
Layer Chromatography ◽  
Chloroform Methanol

The rapid, highly-sensitive and ecologically greener reversed-phase (RP)/normal-phase (NP) high-performance thin-layer chromatography (HPTLC) densitometric technique has been developed and validated for the determination of trans-resveratrol (TRV). The reversed-phase HPTLC-based analysis of TRV was performed using ethanol–water (65:35, v v−1) combination as the greener mobile phase, while, the normal-phase HPTLC-based estimation of TRV was performed using chloroform–methanol (85:15, v v−1) combination as the routine mobile phase. The TRV detection was carried out at 302 nm for RP/NP densitometric assay. The linearity was recorded as 10–1200 and 30–400 ng band−1 for RP and NP HPTLC techniques, respectively. The RP densitometric assay was observed as highly-sensitive, accurate, precise and robust for TRV detection in comparison with the NP densitometric assay. The contents of TRV in commercial formulation were recorded as 101.21% utilizing the RP densitometric assay, while, the contents of TRV in commercial formulation were found to be 91.64% utilizing the NP densitometric assay. The greener profile of RP/NP technique was obtained using the analytical GREEnness (AGREE) approach. The AGREE scales for RP and NP densitometric assays were estimated 0.75 and 0.48, respectively. The recorded AGREE scale for the RP densitometric assay indicated that this technique was highly green/the ecologically greener compared to the NP densitometric assay. After successful optimization of analytical conditions, validation parameters, AGREE scale and chromatography performance, the RP densitometric assay with univariate calibration was found to be better than the NP densitometric assay for the analysis of TRV.

scholarly journals Simultaneous Determination of Caffeine and Paracetamol in Commercial Formulations Using Greener Normal-Phase and Reversed-Phase HPTLC Methods: A Contrast of Validation Parameters

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 405
Author(s):  
Prawez Alam ◽  
Faiyaz Shakeel ◽  
Abuzer Ali ◽  
Mohammed H. Alqarni ◽  
Ahmed I. Foudah ◽  
...  
Keyword(s):  
Thin Layer ◽  
Simultaneous Determination ◽  
High Performance ◽  
Analytical Techniques ◽  
Reversed Phase ◽  
Normal Phase ◽  
Validation Parameters ◽  
Analytical Approaches ◽  
Layer Chromatography

There has been no assessment of the greenness of the described analytical techniques for the simultaneous determination (SMD) of caffeine and paracetamol. As a result, in comparison to the greener normal-phase high-performance thin-layer chromatography (HPTLC) technique, this research was conducted to develop a rapid, sensitive, and greener reversed-phase HPTLC approach for the SMD of caffeine and paracetamol in commercial formulations. The greenness of both techniques was calculated using the AGREE method. For the SMD of caffeine and paracetamol, the greener normal-phase and reversed-phase HPTLC methods were linear in the 50–500 ng/band and 25–800 ng/band ranges, respectively. For the SMD of caffeine and paracetamol, the greener reversed-phase HPTLC approach was more sensitive, accurate, precise, and robust than the greener normal-phase HPTLC technique. For the SMD of caffeine paracetamol in commercial PANEXT and SAFEXT tablets, the greener reversed-phase HPTLC technique was superior to the greener normal-phase HPTLC approach. The AGREE scores for the greener normal-phase and reversed-phase HPTLC approaches were estimated as 0.81 and 0.83, respectively, indicated excellent greenness profiles for both analytical approaches. The greener reversed-phase HPTLC approach is judged superior to the greener normal-phase HPTLC approach based on numerous validation parameters and pharmaceutical assays.

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