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  1. Article ; Online: Novel dummy molecularly imprinted polymer for simultaneous solid-phase extraction of stanozolol metabolites from urine.

    Farag, Yomna G / Hanafi, Rasha S / Hammam, Mennatallah A

    Analytical and bioanalytical chemistry

    2024  

    Abstract: Stanozolol, a synthetic derivative of testosterone, is one of the common doping drugs among athletes and bodybuilders. It is metabolized to a large extent and metabolites are detected in urine for a longer duration than the parent compound. In this study, ...

    Abstract Stanozolol, a synthetic derivative of testosterone, is one of the common doping drugs among athletes and bodybuilders. It is metabolized to a large extent and metabolites are detected in urine for a longer duration than the parent compound. In this study, a novel dummy molecularly imprinted polymer (DMIP) is developed as a sorbent for solid-phase extraction of stanozolol metabolites from spiked human urine samples. The optimized DMIP is composed of stanozolol as the dummy template, methacrylic acid as the functional monomer, and ethylene glycol dimethacrylate as the cross-linker in a ratio of 1:10:80. The extracted analytes were quantitively determined using a newly developed and validated ultrahigh-performance liquid chromatography tandem mass spectrometry method, where the limits of detection and quantitation were 0.91 and 1.81 ng mL
    Language English
    Publishing date 2024-04-25
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 201093-8
    ISSN 1618-2650 ; 0016-1152 ; 0372-7920
    ISSN (online) 1618-2650
    ISSN 0016-1152 ; 0372-7920
    DOI 10.1007/s00216-024-05285-x
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  2. Article ; Online: Kinetic degradation study for the first licensed anti-influenza polymerase inhibitor, baloxavir marboxil, using high-performance liquid chromatography-mass spectrometry.

    Hafez, Hani M / Abdel-Halim, Mohammad / Hemdan, Ahmed / Hammam, Mennatallah A

    Journal of separation science

    2022  Volume 45, Issue 14, Page(s) 2488–2497

    Abstract: The first licensed polymerase inhibitor, baloxavir marboxil was recently approved for the treatment of influenza A and B viruses. Furthermore, there is growing interest in testing the antiviral activity of baloxavir marboxil against Coronavirus. Despite ... ...

    Abstract The first licensed polymerase inhibitor, baloxavir marboxil was recently approved for the treatment of influenza A and B viruses. Furthermore, there is growing interest in testing the antiviral activity of baloxavir marboxil against Coronavirus. Despite its critical clinical value, there is no information on the degradation products, pathways, or kinetics of baloxavir marboxil under various stress conditions. In this study, a new high-performance liquid chromatography-ultraviolet detection method for accurately quantifying baloxavir marboxil in the presence of its degradation products was developed. A study of degradation kinetics revealed that acidic, thermal neutral, and photolytic degradation reactions have zero-order kinetics, whereas basic and oxidative degradation reactions have first-order kinetics. The structural characterization of baloxavir marboxil degradation products was performed by coupling the optimized high-performance liquid chromatography method to the triple-quadrupole tandem mass spectrometer. The proposed approach was validated according to the International Council for Harmonisation Q2 (R1) requirements for accuracy, precision, robustness, specificity, and linearity. The validated new method was successfully used to analyze baloxavir marboxil as raw material and its pharmaceutical dosage form, Xofluza.
    MeSH term(s) Antiviral Agents/therapeutic use ; Chromatography, High Pressure Liquid ; Dibenzothiepins ; Humans ; Influenza, Human/drug therapy ; Mass Spectrometry ; Morpholines ; Oxazines/therapeutic use ; Pyridines ; Pyridones ; Thiepins/therapeutic use ; Triazines
    Chemical Substances Antiviral Agents ; Dibenzothiepins ; Morpholines ; Oxazines ; Pyridines ; Pyridones ; Thiepins ; Triazines ; baloxavir (4G86Y4JT3F)
    Language English
    Publishing date 2022-05-20
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2047990-6
    ISSN 1615-9314 ; 1615-9306
    ISSN (online) 1615-9314
    ISSN 1615-9306
    DOI 10.1002/jssc.202200020
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  3. Article: Kinetic degradation study for the first licensed anti‐influenza polymerase inhibitor, baloxavir marboxil, using high‐performance liquid chromatography‐mass spectrometry

    Hafez, Hani M. / Abdel‐Halim, Mohammad / Hemdan, Ahmed / Hammam, Mennatallah A.

    Journal of separation science. 2022 July, v. 45, no. 14

    2022  

    Abstract: The first licensed polymerase inhibitor, baloxavir marboxil was recently approved for the treatment of influenza A and B viruses. Furthermore, there is growing interest in testing the antiviral activity of baloxavir marboxil against Coronavirus. Despite ... ...

    Abstract The first licensed polymerase inhibitor, baloxavir marboxil was recently approved for the treatment of influenza A and B viruses. Furthermore, there is growing interest in testing the antiviral activity of baloxavir marboxil against Coronavirus. Despite its critical clinical value, there is no information on the degradation products, pathways, or kinetics of baloxavir marboxil under various stress conditions. In this study, a new high‐performance liquid chromatography‐ultraviolet detection method for accurately quantifying baloxavir marboxil in the presence of its degradation products was developed. A study of degradation kinetics revealed that acidic, thermal neutral, and photolytic degradation reactions have zero‐order kinetics, whereas basic and oxidative degradation reactions have first‐order kinetics. The structural characterization of baloxavir marboxil degradation products was performed by coupling the optimized high‐performance liquid chromatography method to the triple‐quadrupole tandem mass spectrometer. The proposed approach was validated according to the International Council for Harmonisation Q2 (R1) requirements for accuracy, precision, robustness, specificity, and linearity. The validated new method was successfully used to analyze baloxavir marboxil as raw material and its pharmaceutical dosage form, Xofluza.
    Keywords Orthocoronavirinae ; antiviral properties ; dosage forms ; high performance liquid chromatography ; influenza ; mass spectrometry ; photolysis ; raw materials ; separation ; spectrometers
    Language English
    Dates of publication 2022-07
    Size p. 2488-2497.
    Publishing place John Wiley & Sons, Ltd
    Document type Article
    Note JOURNAL ARTICLE
    ZDB-ID 2047990-6
    ISSN 1615-9314 ; 1615-9306
    ISSN (online) 1615-9314
    ISSN 1615-9306
    DOI 10.1002/jssc.202200020
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  4. Article ; Online: From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.

    Abdel-Halim, Mohammad / Sigler, Sara / Racheed, Nora A S / Hefnawy, Amr / Fathalla, Reem K / Hammam, Mennatallah A / Maher, Ahmed / Maxuitenko, Yulia / Keeton, Adam B / Hartmann, Rolf W / Engel, Matthias / Piazza, Gary A / Abadi, Ashraf H

    Journal of medicinal chemistry

    2021  Volume 64, Issue 8, Page(s) 4462–4477

    Abstract: A ligand-based approach involving systematic modifications of a trisubstituted pyrazoline scaffold derived from the COX2 inhibitor, celecoxib, was used to develop novel PDE5 inhibitors. Novel pyrazolines were identified with potent PDE5 inhibitory ... ...

    Abstract A ligand-based approach involving systematic modifications of a trisubstituted pyrazoline scaffold derived from the COX2 inhibitor, celecoxib, was used to develop novel PDE5 inhibitors. Novel pyrazolines were identified with potent PDE5 inhibitory activity lacking COX2 inhibitory activity. Compound
    MeSH term(s) Animals ; Blood Proteins/chemistry ; Blood Proteins/metabolism ; Celecoxib/chemistry ; Celecoxib/metabolism ; Cyclic Nucleotide Phosphodiesterases, Type 5/chemistry ; Cyclic Nucleotide Phosphodiesterases, Type 5/genetics ; Cyclic Nucleotide Phosphodiesterases, Type 5/metabolism ; Drug Design ; Female ; Half-Life ; Humans ; Isoenzymes/antagonists & inhibitors ; Isoenzymes/metabolism ; Mice ; Mice, Inbred C57BL ; Microsomes, Liver/metabolism ; Phosphodiesterase 5 Inhibitors/chemistry ; Phosphodiesterase 5 Inhibitors/metabolism ; Protein Binding ; Pyrazoles/chemistry ; Pyrazoles/metabolism ; Recombinant Proteins/biosynthesis ; Recombinant Proteins/chemistry ; Stereoisomerism ; Structure-Activity Relationship
    Chemical Substances Blood Proteins ; Isoenzymes ; Phosphodiesterase 5 Inhibitors ; Pyrazoles ; Recombinant Proteins ; Cyclic Nucleotide Phosphodiesterases, Type 5 (EC 3.1.4.35) ; Celecoxib (JCX84Q7J1L)
    Language English
    Publishing date 2021-04-01
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.0c01120
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    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
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  5. Article ; Online: Discovery of trisubstituted pyrazolines as a novel scaffold for the development of selective phosphodiesterase 5 inhibitors.

    Abdel-Halim, Mohammad / Tinsley, Heather / Keeton, Adam B / Weam, Mohammed / Atta, Noha H / Hammam, Mennatallah A / Hefnawy, Amr / Hartmann, Rolf W / Engel, Matthias / Piazza, Gary A / Abadi, Ashraf H

    Bioorganic chemistry

    2020  Volume 104, Page(s) 104322

    Abstract: Celecoxib, is a selective cyclooxygenase-2 (COX2) inhibitor with a 1,5-diaryl pyrazole scaffold. Celecoxib has a better safety profile compared to other COX2 inhibitors having side effects of systemic hypertension and thromboembolic complications. This ... ...

    Abstract Celecoxib, is a selective cyclooxygenase-2 (COX2) inhibitor with a 1,5-diaryl pyrazole scaffold. Celecoxib has a better safety profile compared to other COX2 inhibitors having side effects of systemic hypertension and thromboembolic complications. This may be partly attributed to an off-target activity involving phosphodiesterase 5 (PDE5) inhibition and the potentiation of NO/cGMP signalling allowing coronary vasodilation and aortic relaxation. Inspired by the structure of celecoxib, we synthesized a chemically diverse series of compounds containing a 1,3,5-trisubstituted pyrazoline scaffold to improve PDE5 inhibitory potency, while eliminating COX2 inhibitory activity. SAR studies for PDE5 inhibition revealed an essential role for a carboxylic acid functionality at the 1-phenyl and the importance of the non-planar pyrazoline core over the planar pyrazole with the 5-phenyl moiety tolerating a range of substituents. These modifications led to new PDE5 inhibitors with approximately 20-fold improved potency to inhibit PDE5 and no COX-2 inhibitory activity compared with celecoxib. PDE isozyme profiling of compound 11 revealed a favorable selectivity profile. These results suggest that trisubstituted pyrazolines provide a promising scaffold for further chemical optimization to identify novel PDE5 inhibitors with potential for less side effects compared with available PDE5 inhibitors used for the treatment of penile erectile dysfunction and pulmonary hypertension.
    MeSH term(s) Cyclic Nucleotide Phosphodiesterases, Type 5/metabolism ; Dose-Response Relationship, Drug ; Drug Discovery ; Humans ; Molecular Structure ; Phosphodiesterase 5 Inhibitors/chemical synthesis ; Phosphodiesterase 5 Inhibitors/chemistry ; Phosphodiesterase 5 Inhibitors/pharmacology ; Pyrazoles/chemical synthesis ; Pyrazoles/chemistry ; Pyrazoles/pharmacology ; Structure-Activity Relationship
    Chemical Substances Phosphodiesterase 5 Inhibitors ; Pyrazoles ; pyrazole (3QD5KJZ7ZJ) ; Cyclic Nucleotide Phosphodiesterases, Type 5 (EC 3.1.4.35)
    Language English
    Publishing date 2020-09-28
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2020.104322
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