Miloš Sedlák

Summary

Affiliation: University of Pardubice
Country: Czech Republic

Publications

  1. doi request reprint Synthesis and characterization of a pH-sensitive conjugate of isoniazid with Fe3O4@SiO2 magnetic nanoparticles
    Miloš Sedlák
    Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Bioorg Med Chem Lett 23:4692-5. 2013
  2. ncbi request reprint Synthesis and characterisation of a new pH-sensitive amphotericin B--poly(ethylene glycol)-b-poly(L-lysine) conjugate
    Miloš Sedlák
    Department of Organic Chemistry, University of Pardubice, Pardubice, Czech Republic
    Bioorg Med Chem Lett 17:2554-7. 2007
  3. ncbi request reprint Amphotericin B: from derivatives to covalent targeted conjugates
    Miloš Sedlák
    Department of Organic Chemistry and Technology, University of Pardubice, The Czech Republic
    Mini Rev Med Chem 9:1306-16. 2009
  4. doi request reprint New targeting system for antimycotic drugs: beta-glucosidase sensitive amphotericin B-star poly(ethylene glycol) conjugate
    Miloš Sedlák
    Department of Organic Chemistry, Faculty of Chemical Technology, University of Pardubice, Cs legií 565, 532 10 Pardubice, Czech Republic
    Bioorg Med Chem Lett 18:2952-6. 2008
  5. ncbi request reprint Synthesis of pH-sensitive amphotericin B-poly(ethylene glycol) conjugates and study of their controlled release in vitro
    Miloš Sedlák
    Department of Organic Chemistry, University of Pardubice, Cs legií 565, 532 10 Pardubice, Czech Republic
    Bioorg Med Chem 15:4069-76. 2007
  6. doi request reprint Targeted antifungal delivery system: beta-glucosidase sensitive nystatin-star poly(ethylene glycol) conjugate
    Eliška Bílková
    Department of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Int J Pharm 386:1-5. 2010
  7. doi request reprint Prednisolone-α-cyclodextrin-star poly(ethylene glycol) polypseudorotaxane with delayed pH-sensitivity as a targeted drug delivery system
    Eliška Bílková
    Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Int J Pharm 414:42-7. 2011
  8. doi request reprint Synthesis and characterization of pH-sensitive conjugate of isoniazid--methoxypoly(ethylene glycol)-b-poly(L-lysine)
    Ales Imramovsky
    Institute of Organic Chemistry and Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Bioorg Med Chem Lett 22:5952-5. 2012
  9. doi request reprint Inverse neighboring group participation: explanation of an unusual S→N alkyl migration of isothiuronium salts containing a lactone group
    Jirí Vána
    Faculty of Chemical Technology, Institute of Organic Chemistry and Technology, University of Pardubice, Studentska 573, CZ 532 10 Pardubice, The Czech Republic
    J Org Chem 78:4456-62. 2013
  10. ncbi request reprint Recent advances in the design and synthesis of prednisolone and methylprednisolone conjugates
    Eliška Bílková
    Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Curr Pharm Des 17:3577-95. 2011

Collaborators

Detail Information

Publications13

  1. doi request reprint Synthesis and characterization of a pH-sensitive conjugate of isoniazid with Fe3O4@SiO2 magnetic nanoparticles
    Miloš Sedlák
    Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Bioorg Med Chem Lett 23:4692-5. 2013
    ..The conjugate released isoniazid under in vitro conditions (pH=4; 37 °C; t1/2≈115 s). In addition, the cytotoxicity of the Fe3O4@SiO2-INH conjugate was evaluated in SK-BR-3 cells using the xCELLigence system...
  2. ncbi request reprint Synthesis and characterisation of a new pH-sensitive amphotericin B--poly(ethylene glycol)-b-poly(L-lysine) conjugate
    Miloš Sedlák
    Department of Organic Chemistry, University of Pardubice, Pardubice, Czech Republic
    Bioorg Med Chem Lett 17:2554-7. 2007
    ..4, 37 degrees C). Controlled release of AMB was observed in acidic phosphate buffer (pH 5.5, 37 degrees C) with the half-life of 2 min. The LD(50) value determined in vivo (mouse) is 45 mg/kg...
  3. ncbi request reprint Amphotericin B: from derivatives to covalent targeted conjugates
    Miloš Sedlák
    Department of Organic Chemistry and Technology, University of Pardubice, The Czech Republic
    Mini Rev Med Chem 9:1306-16. 2009
    ..The examples presented include variation of functional groups in AMB, covalent conjugates with other molecules, poly(ethylene glycols) and polysaccharides. Possibilities of targeted delivery of AMB are discussed...
  4. doi request reprint New targeting system for antimycotic drugs: beta-glucosidase sensitive amphotericin B-star poly(ethylene glycol) conjugate
    Miloš Sedlák
    Department of Organic Chemistry, Faculty of Chemical Technology, University of Pardubice, Cs legií 565, 532 10 Pardubice, Czech Republic
    Bioorg Med Chem Lett 18:2952-6. 2008
    ..C.3.2.1.21). The beta-glucosidase-catalyzed release of AMB from the polymeric carrier was proved in vitro by means of spectrophotometry and HPLC...
  5. ncbi request reprint Synthesis of pH-sensitive amphotericin B-poly(ethylene glycol) conjugates and study of their controlled release in vitro
    Miloš Sedlák
    Department of Organic Chemistry, University of Pardubice, Cs legií 565, 532 10 Pardubice, Czech Republic
    Bioorg Med Chem 15:4069-76. 2007
    ..The LD50 values determined in vivo (mouse) are 20.7 mg/kg and 40.5 mg/kg for the conjugates with ester linkage (M = 10,000 and 5000, respectively), which means that they are ca. 6-11 times less toxic than free AMB...
  6. doi request reprint Targeted antifungal delivery system: beta-glucosidase sensitive nystatin-star poly(ethylene glycol) conjugate
    Eliška Bílková
    Department of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Int J Pharm 386:1-5. 2010
    ..6 units/g; pH 7.4, 2 x 10(-2)M), reported decomposition half-life of conjugate tau(1/2)=(88+/-2)s. This implies that releasing of nystatin is controlled only enzymatically...
  7. doi request reprint Prednisolone-α-cyclodextrin-star poly(ethylene glycol) polypseudorotaxane with delayed pH-sensitivity as a targeted drug delivery system
    Eliška Bílková
    Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Int J Pharm 414:42-7. 2011
    ..The prepared polypseudorotaxane represents a promising peroral transport system of prednisolone with a pH-sensitive linker with delayed acid-catalysed hydrolysis thanks to protection at the molecular level using α-cyclodextrin...
  8. doi request reprint Synthesis and characterization of pH-sensitive conjugate of isoniazid--methoxypoly(ethylene glycol)-b-poly(L-lysine)
    Ales Imramovsky
    Institute of Organic Chemistry and Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Bioorg Med Chem Lett 22:5952-5. 2012
    ..Under in vitro conditions, the conjugate is hydrolyzed and isoniazid is released (pH 4; 37 °C; t(1/2) ≈ 10 h)...
  9. doi request reprint Inverse neighboring group participation: explanation of an unusual S→N alkyl migration of isothiuronium salts containing a lactone group
    Jirí Vána
    Faculty of Chemical Technology, Institute of Organic Chemistry and Technology, University of Pardubice, Studentska 573, CZ 532 10 Pardubice, The Czech Republic
    J Org Chem 78:4456-62. 2013
    ..It was found that the intermediate has a structure of a free ion pair. The double-displacement mechanism can be considered as a new type of inverse lactone neighboring group participation...
  10. ncbi request reprint Recent advances in the design and synthesis of prednisolone and methylprednisolone conjugates
    Eliška Bílková
    Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Curr Pharm Des 17:3577-95. 2011
    ..These two groups are further divided into subgroups based on the chemical structure of the conjugates. Published results from in vitro and in vivo testing of prepared conjugates are also discussed...
  11. doi request reprint Prednisolone-α-cyclodextrin-star PEG polypseudorotaxanes with controlled drug delivery properties
    Eliška Bílková
    Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic
    Org Biomol Chem 8:5423-30. 2010
    ..The synthesized polypseudorotaxanes represent new promising transport systems intended for targeted release of prednisolone in transplanted liver...
  12. ncbi request reprint Highly enantioselective nitroaldol reactions catalyzed by copper(II) complexes derived from substituted 2-(pyridin-2-yl)imidazolidin-4-one ligands
    Illia Panov
    Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Pardubice, Czech Republic
    J Org Chem 76:4787-93. 2011
    ..In the case of an anti arrangement of the imidazolidin-4-one ring, the obtained result was 91-96% ee, whereas in the case of syn arrangement, a significant drop to 25-27% ee was observed...
  13. doi request reprint Kinetic evidence for the coexistence of zwitterionic (T+/-), neutral (T0) and anionic (T-) intermediates during rearrangement of S-(2-oxotetrahydrofuran-3-yl)-N-(4-methoxyphenyl)isothiuronium bromide to 5-(2-hydroxyethyl)-2-(4-methoxyphenylimino)-1,3-thia
    Jirí Vána
    Faculty of Chemical Technology, Institute of Organic Chemistry and Technology, University of Pardubice, CZ 532 10 Pardubice, The Czech Republic
    J Org Chem 75:3729-36. 2010
    ..Coexistence of all three kinetically detectable intermediates is very rare and is possibly due to relatively enhanced stability of these intermediates necessitating participation of an acid for progression to products...