Paul Gleeson, Matthew

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Paul Gleeson, Matthew
Alternative Name
Paul Gleeson, M.
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Email
paul.gl@kmitl.ac.th

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    Item type:Publication,
    Assessment of the Utility of Chitosan in Drug Delivery of Sulfamethoxazole
    (2024-01-01)
    Soontorntepwarakul, Nussara
    ;
    Boonyarattanakalin, Kanokthip
    ;
    Srirussamee, Kasama
    ;
    Paul Gleeson, M.
    The objective of this research was to develop chitosan (CS) nanoparticles (NP) and microfibres (MF) for oral delivery applications related to low solubility drugs. The ionic gelation method in conjunction with freeze-drying was used to produce crosslinked chitosan material. Dynamic light scattering (DLS) was used to characterize particle size and polydispersity index (PDI). Surface morphology was analyzed using scanning electron microscopy (SEM). The antibiotic drug sulfamethoxazole (SMO) was loaded onto the chitosan nano/micro material. The degree of loading, loading efficiency and the release kinetics were investigated using high-performance liquid chromatography (HPLC) and UV-visible spectrophotometry, respectively. We found that CS nanoparticles have the potential to improve the delivery properties of SMO due to their more rapid release compared to microfibres or traditional tablet formulations.
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    Item type:Publication,
    Computational design, synthesis and biological evaluation of PDE5 inhibitors based on N2,N4-diaminoquinazoline and N2,N6-diaminopurine scaffolds
    (2022-12-15)
    Somnarin, Thanachon
    ;
    Pobsuk, Nattakarn
    ;
    Chantakul, Ruttanaporn
    ;
    Panklai, Teerapap
    ;
    Temkitthawon, Prapapan
    We report the synthesis, and characterization of twenty-nine new inhibitors of PDE5. Structure-based design was employed to modify to our previously reported 2,4-diaminoquinazoline series. Modification include scaffold hopping to 2,6-diaminopurine core as well as incorporation of ionizable groups to improve both activity and solubility. The prospective binding mode of the compounds was determined using 3D ligand-based similarity methods to inhibitors of known binding mode, combined with a PDE5 docking and molecular dynamics based-protocol, each of which pointed to the same binding mode. Chemical modifications were then designed to both increase potency and solubility as well as validate the binding mode prediction. Compounds containing a quinazoline core displayed IC<inf>50</inf>s ranging from 0.10 to 9.39 µM while those consisting of a purine scaffold ranging from 0.29 to 43.16 µM. We identified 25 with a PDE5 IC<inf>50</inf> of 0.15 µM, and much improved solubility (1.77 mg/mL) over the starting lead. Furthermore, it was found that the predicted binding mode was consistent with the observed SAR validating our computationally driven approach.