A+ synthesis of erythromycin and rapamycin | …

This latter process accomplished in one step the installation of the remaining two carbons of the natural product and the completion of its total synthesis.">

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The biosynthetic genes responsible for rapamycin synthesis have been identified

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T1 - Synthesis, characterization and antiproliferative activity of rapamycin-loaded poly(N-isopropylacrylamide)-based nanogels in vascular smooth muscle cells

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N2 - Nanogels consist of three-dimensional cross-linked macromolecular polymeric networks which can be loaded with drugs for sustained delivery. In this study, nanogels comprising of poly(N-isopropylacrylamide) (PNIPAM) (NG-1), PNIPAM with poly(ethylene glycol)-maleic anhydride (PEG-MA) (NG-2), and PNIPAM and vinyl pyrrolidone (VP) with PEG-MA (NG-3) were synthesized using simultaneous free-radical cross-linking polymerization in the presence of N,N′-methylenebisacrylamide (cross-linker) and ammonium persulphate/ferrous ammonium sulphate (initiating pair). The chemical constituents present in nanogels were confirmed by spectral analysis (FT-IR, 1H-NMR). The inherent phase transition property of nanogels was determined by measuring lower critical solution temperature (LCST) using UV-Vis spectrophotometer. Rapamycin was selected for loading into nanogels because of our interest in using the drug-loaded nanogel formulations for intravascular drug delivery to prevent post-angioplasty restenosis. Size of nanogels ranged from 25-28 nm in diameter by transmission electron microscopy whereas it ranged from 35-45 nm when determined using dynamic light scattering. Nanogels demonstrated the drug loading capacity (NG-3 > NG-2 ≥ NG-1) and release (NG-1 > NG-2 > NG-3) which varied with the chemical composition of nanogels. NG-1 showed LCST ot 38 °C whereas the modified nanogels i.e., NG-2 and NG-3 showed 39 °C and 55 °C, respectively. Nanogels were compatible with vascular smooth muscle cells (VSMCs) and the anti-proliferative effect of the drug loaded nanogels was dose-dependent. Thus, nanogels can be used for intravascular delivery of rapamycin, which is an insoluble drug, and hence can not be administered intravenously.

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Total Synthesis of Rapamycin - ResearchGate

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This latter process accomplished in one step the installation of the remaining two carbons of the natural product and the completion of its total synthesis.

Synthesis of rapamycin glycoconjugates via a CuAAC …

Regiospecific synthesis of rapamycin 42 ..

Nanogels consist of three-dimensional cross-linked macromolecular polymeric networks which can be loaded with drugs for sustained delivery. In this study, nanogels comprising of poly(N-isopropylacrylamide) (PNIPAM) (NG-1), PNIPAM with poly(ethylene glycol)-maleic anhydride (PEG-MA) (NG-2), and PNIPAM and vinyl pyrrolidone (VP) with PEG-MA (NG-3) were synthesized using simultaneous free-radical cross-linking polymerization in the presence of N,N′-methylenebisacrylamide (cross-linker) and ammonium persulphate/ferrous ammonium sulphate (initiating pair). The chemical constituents present in nanogels were confirmed by spectral analysis (FT-IR, 1H-NMR). The inherent phase transition property of nanogels was determined by measuring lower critical solution temperature (LCST) using UV-Vis spectrophotometer. Rapamycin was selected for loading into nanogels because of our interest in using the drug-loaded nanogel formulations for intravascular drug delivery to prevent post-angioplasty restenosis. Size of nanogels ranged from 25-28 nm in diameter by transmission electron microscopy whereas it ranged from 35-45 nm when determined using dynamic light scattering. Nanogels demonstrated the drug loading capacity (NG-3 > NG-2 ≥ NG-1) and release (NG-1 > NG-2 > NG-3) which varied with the chemical composition of nanogels. NG-1 showed LCST ot 38 °C whereas the modified nanogels i.e., NG-2 and NG-3 showed 39 °C and 55 °C, respectively. Nanogels were compatible with vascular smooth muscle cells (VSMCs) and the anti-proliferative effect of the drug loaded nanogels was dose-dependent. Thus, nanogels can be used for intravascular delivery of rapamycin, which is an insoluble drug, and hence can not be administered intravenously.

A method for the regiospecific synthesis of rapamycin 42-ester derivatives is described

Synthesis of Dienylstannane D ..

AB - Nanogels consist of three-dimensional cross-linked macromolecular polymeric networks which can be loaded with drugs for sustained delivery. In this study, nanogels comprising of poly(N-isopropylacrylamide) (PNIPAM) (NG-1), PNIPAM with poly(ethylene glycol)-maleic anhydride (PEG-MA) (NG-2), and PNIPAM and vinyl pyrrolidone (VP) with PEG-MA (NG-3) were synthesized using simultaneous free-radical cross-linking polymerization in the presence of N,N′-methylenebisacrylamide (cross-linker) and ammonium persulphate/ferrous ammonium sulphate (initiating pair). The chemical constituents present in nanogels were confirmed by spectral analysis (FT-IR, 1H-NMR). The inherent phase transition property of nanogels was determined by measuring lower critical solution temperature (LCST) using UV-Vis spectrophotometer. Rapamycin was selected for loading into nanogels because of our interest in using the drug-loaded nanogel formulations for intravascular drug delivery to prevent post-angioplasty restenosis. Size of nanogels ranged from 25-28 nm in diameter by transmission electron microscopy whereas it ranged from 35-45 nm when determined using dynamic light scattering. Nanogels demonstrated the drug loading capacity (NG-3 > NG-2 ≥ NG-1) and release (NG-1 > NG-2 > NG-3) which varied with the chemical composition of nanogels. NG-1 showed LCST ot 38 °C whereas the modified nanogels i.e., NG-2 and NG-3 showed 39 °C and 55 °C, respectively. Nanogels were compatible with vascular smooth muscle cells (VSMCs) and the anti-proliferative effect of the drug loaded nanogels was dose-dependent. Thus, nanogels can be used for intravascular delivery of rapamycin, which is an insoluble drug, and hence can not be administered intravenously.