A series of near-infrared (NIR) fluorochromes with large Stokes shifts was designed, synthesized, and evaluated for application in non-invasive imaging of tumor hypoxia. Each NIR fluorescent hypoxia probe comprised a tricarbocyanine dye and a 2-nitroimidazole-containing moiety as a hypoxia marker that binds to cellular nucleophiles via bioreductive activation under hypoxic conditions. Nucleophilic displacement of the amino-nucleophilic linker moiety of heptamethine cyanine dyes having a 2-chloro-1-cyclohexenyl ring and a 2-nitroimidazole moiety yielded various fluorochromes with different hydrophilicity. These exhibited long emission wavelengths (747–758 nm) with large Stokes shifts (111–125 nm) and high quantum yield (0.04–0.34). GPU-210, 297, and 316 showed significantly higher levels of fluorescence under hypoxic than under normoxic conditions on treating SUIT-2/HRE-Luc pancreatic cancer cells. Among these, only GPU-316 showed significant fluorescence intensity in tumor tissue in in vivo fluorescence imaging of mouse xenograft models.

A series of near-infrared (NIR) fluorochromes with large Stokes shifts was designed, synthesized, and evaluated for application in non-invasive imaging of tumor hypoxia. Each NIR fluorescent hypoxia probe comprised a tricarbocyanine dye and a 2-nitroimidazole-containing moiety as a hypoxia marker that binds to cellular nucleophiles via bioreductive activation under hypoxic conditions. Nucleophilic displacement of the amino-nucleophilic linker moiety of heptamethine cyanine dyes having a 2-chloro-1-cyclohexenyl ring and a 2-nitroimidazole moiety yielded various fluorochromes with different hydrophilicity. These exhibited long emission wavelengths (747–758 nm) with large Stokes shifts (111–125 nm) and high quantum yield (0.04–0.34). GPU-210, 297, and 316 showed significantly higher levels of fluorescence under hypoxic than under normoxic conditions on treating SUIT-2/HRE-Luc pancreatic cancer cells. Among these, only GPU-316 showed significant fluorescence intensity in tumor tissue in in vivo fluorescence imaging of mouse xenograft models.

A series of near-infrared (NIR) fluorochromes with large Stokes shifts was designed, synthesized, and evaluated for application in non-invasive imaging of tumor hypoxia. Each NIR fluorescent hypoxia probe comprised a tricarbocyanine dye and a 2-nitroimidazole-containing moiety as a hypoxia marker that binds to cellular nucleophiles via bioreductive activation under hypoxic conditions. Nucleophilic displacement of the amino-nucleophilic linker moiety of heptamethine cyanine dyes having a 2-chloro-1-cyclohexenyl ring and a 2-nitroimidazole moiety yielded various fluorochromes with different hydrophilicity. These exhibited long emission wavelengths (747–758 nm) with large Stokes shifts (111–125 nm) and high quantum yield (0.04–0.34). GPU-210, 297, and 316 showed significantly higher levels of fluorescence under hypoxic than under normoxic conditions on treating SUIT-2/HRE-Luc pancreatic cancer cells. Among these, only GPU-316 showed significant fluorescence intensity in tumor tissue in in vivo fluorescence imaging of mouse xenograft models.

A series of near-infrared (NIR) fluorochromes with large Stokes shifts was designed, synthesized, and evaluated for application in non-invasive imaging of tumor hypoxia. Each NIR fluorescent hypoxia probe comprised a tricarbocyanine dye and a 2-nitroimidazole-containing moiety as a hypoxia marker that binds to cellular nucleophiles via bioreductive activation under hypoxic conditions. Nucleophilic displacement of the amino-nucleophilic linker moiety of heptamethine cyanine dyes having a 2-chloro-1-cyclohexenyl ring and a 2-nitroimidazole moiety yielded various fluorochromes with different hydrophilicity. These exhibited long emission wavelengths (747–758 nm) with large Stokes shifts (111–125 nm) and high quantum yield (0.04–0.34). GPU-210, 297, and 316 showed significantly higher levels of fluorescence under hypoxic than under normoxic conditions on treating SUIT-2/HRE-Luc pancreatic cancer cells. Among these, only GPU-316 showed significant fluorescence intensity in tumor tissue in in vivo fluorescence imaging of mouse xenograft models.

Background: Lipophilicity is a physicochemical property of an essential importance in medicinal chemistry; therefore, fast and reliable measurement of lipophilicity will affect greatly the drug discovery process. Results: A series of N-benzenesulfonamide-1H-pyrazoles, oximes and hydrazones as celecoxib analogues was investigated with regard to their retention behavior using reversed-phase high performance liquid chromatography (RPHPLC). The mobile phases employed for this study consist of a mixture of water and methanol in different proportions. In addition, the stationary phase utilized for this separation was C18 silanized silica gel and using 200 nm as a detection wavelength. The retention behavior of the investigated compounds was determined based on practical determination of log k at different concentrations of methanol (as an organic modifier) in the mobile phase ranging from 60 to 80%. It was observed that the retention of these compounds (expressed as log k) decreased in a linear manner with increasing the concentration of methanol. High correlation coefficients (more than 0.90 in most cases) were obtained for the relationship between the volume fraction of the organic solvent and the retention values represented as log kw. A comparative evaluation was carried out between chromatographically-obtained lipophilicity parameters (represented as lipophilicity chromatographic index log kw or isocratic chromatographic hydrophobicity index, 0) and the computationally calculated log P values (miLogP, ALOGP, ACD/Labs and ALOGPs). Conclusion: It was found that a good correlation exists between the experimental and computed log P values. In the future, these results

The presented study aims to develop a new online enrichment strategy [“pseudostationary ion-exchanger” (PSIE) sweeping] for the analysis of highly hydrophilic nucleosides in urine samples with a special focus on the fundamental aspects regarding the enrichment process itself. In the first method, we employ the ionic liquid (IL)-type surfactant 1-tetradecyl-3-methylimidazolium bromide (C14MImBr) as micelle forming agent under alkaline pH conditions. It is shown that maximum enrichment efficiency can be obtained by keeping the retention factors very high within the sample zone and very low within the background electrolyte (BGE) while maintaining a sufficient resolution for the studied analytes. With this method, detection limits as low as 0.1 µg mL−1 are obtained for all analytes studied. For the nucleosides, adenosine and cytidine, a second method is developed using sodium dodecyl sulfate (SDS) as micelle forming agent under acidic pH conditions. In addition, we investigate the effect of replacing ionic buffering constituents with a zwitterionic/isoelectric buffering compound (aspartic acid) with regard to separation and enrichment efficiency. With the second method, the achieved limits of detection are as low as 0.1 µg mL−1 for Ado and 0.2 µg mL–1 for Cyd. The applicability of the two complementary methods to the analysis of the nucleosides under investigation is shown for blank and spiked human urine samples after their extraction using the commercially available phenylboronate affinity gel.

In the last few decades, many new antiepileptic drugs came out to medicine world, and their use was expanded over a wide range of cases. Analysts from all over the world developed many different separation methods for the determination of these drugs in a quantitative way either in pharmaceutical dosage forms or in biological fluids. In this review article, a summation of previously published separation methods including high-performance thin-layer chromatography, high-performance liquid chromatography, gas chromatography, and electrophoresis used for the determination of eslicarbazepine acetate, levetiracetam, lacosamide, oxcarbazepine, pregabalin, and retigabine are presented. These six drugs are the most commonly used drugs for the treatment of patients diagnosed with partial onset seizures. This article can help researchers and analysts to build upon this knowledge and add further methods of analysis in the future.

In the last few decades, many new antiepileptic drugs came out to medicine world, and their use was expanded over a wide range of cases. Analysts from all over the world developed many different separation methods for the determination of these drugs in a quantitative way either in pharmaceutical dosage forms or in biological fluids. In this review article, a summation of previously published separation methods including high-performance thin-layer chromatography, high-performance liquid chromatography, gas chromatography, and electrophoresis used for the determination of eslicarbazepine acetate, levetiracetam, lacosamide, oxcarbazepine, pregabalin, and retigabine are presented. These six drugs are the most commonly used drugs for the treatment of patients diagnosed with partial onset seizures. This article can help researchers and analysts to build upon this knowledge and add further methods of analysis in the future.

In the last few decades, many new antiepileptic drugs came out to medicine world, and their use was expanded over a wide range of cases. Analysts from all over the world developed many different separation methods for the determination of these drugs in a quantitative way either in pharmaceutical dosage forms or in biological fluids. In this review article, a summation of previously published separation methods including high-performance thin-layer chromatography, high-performance liquid chromatography, gas chromatography, and electrophoresis used for the determination of eslicarbazepine acetate, levetiracetam, lacosamide, oxcarbazepine, pregabalin, and retigabine are presented. These six drugs are the most commonly used drugs for the treatment of patients diagnosed with partial onset seizures. This article can help researchers and analysts to build upon this knowledge and add further methods of analysis in the future.

In the last few decades, many new antiepileptic drugs came out to medicine world, and their use was expanded over a wide range of cases. Analysts from all over the world developed many different separation methods for the determination of these drugs in a quantitative way either in pharmaceutical dosage forms or in biological fluids. In this review article, a summation of previously published separation methods including high-performance thin-layer chromatography, high-performance liquid chromatography, gas chromatography, and electrophoresis used for the determination of eslicarbazepine acetate, levetiracetam, lacosamide, oxcarbazepine, pregabalin, and retigabine are presented. These six drugs are the most commonly used drugs for the treatment of patients diagnosed with partial onset seizures. This article can help researchers and analysts to build upon this knowledge and add further methods of analysis in the future.