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10.1038/srep15216 http://scihub22266oqcxt.onion/10.1038/srep15216 C4604475!4604475!26463125     free     free     free Warning: imagejpeg(C:\Inetpub\vhosts\kidney.de\httpdocs\phplern\26463125.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117       Sci+Rep 2015 ; 5 (ä): ä Nephropedia Template TP {{tp|p=26463125|t=2015. Amino Acid Carbamates As Prodrugs Of Resveratrol |pdf=|usr=}}{{26463125}} gab.com Text Amino Acid Carbamates As Prodrugs Of Resveratrol JO: Sci Rep http://www.kidney.de/pget.php?&tw=1&pmid=26463125 #FOAvip Resveratrol (3, 5, 4?-trihydroxy-trans-stilbene), a plant polyphenol, has important drug-like properties, but its pharmacological exploitation in vivo is hindered by its rapid transformation via phase II conjugative metabolism. One approach to bypass this problem relies on prodrugs. We report here the synthesis, characterization, stability and in vivo pharmacokinetic behaviour of prodrugs of resveratrol in which the OH groups are engaged in an N-monosubstituted carbamate ester (-OC(O)NHR) linkage with a natural amino acid (Leu, Ile, Phe, Thr) to prevent conjugation and modulate the physicochemical properties of the molecule. We also report a convenient, high-yield protocol to obtain derivatives of this type. The new carbamate ester derivatives are stable at pH 1, while they undergo slow hydrolysis at physiological pH and hydrolyse with kinetics suitable for use in prodrugs in whole blood. After administration to rats by oral gavage the isoleucine-containing prodrug was significantly absorbed, and was present in the bloodstream as non-metabolized unaltered or partially deprotected species, demonstrating effective shielding from first-pass metabolism. We conclude that prodrugs based on the N-monosubstituted carbamate ester bond have the appropriate stability profile for the systemic delivery of phenolic compounds. Twit Text FOAVip Amino Acid Carbamates As Prodrugs Of Resveratrol ????Sci Rep http://www.kidney.de/pget.php?&tw=1&pmid=26463125 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=26463125 #FOAvip English Wikipedia <ref>{{Cite pmid|26463125}}</ref> Amino Acid Carbamates As Prodrugs Of Resveratrol #MMPMID26463125 Mattarei A; Azzolini M; La Spina M; Zoratti M; Paradisi C; Biasutto L Sci Rep 2015[]; 5 (ä): ä PMID26463125show ga Resveratrol (3, 5, 4?-trihydroxy-trans-stilbene), a plant polyphenol, has important drug-like properties, but its pharmacological exploitation in vivo is hindered by its rapid transformation via phase II conjugative metabolism. One approach to bypass this problem relies on prodrugs. We report here the synthesis, characterization, stability and in vivo pharmacokinetic behaviour of prodrugs of resveratrol in which the OH groups are engaged in an N-monosubstituted carbamate ester (-OC(O)NHR) linkage with a natural amino acid (Leu, Ile, Phe, Thr) to prevent conjugation and modulate the physicochemical properties of the molecule. We also report a convenient, high-yield protocol to obtain derivatives of this type. The new carbamate ester derivatives are stable at pH 1, while they undergo slow hydrolysis at physiological pH and hydrolyse with kinetics suitable for use in prodrugs in whole blood. After administration to rats by oral gavage the isoleucine-containing prodrug was significantly absorbed, and was present in the bloodstream as non-metabolized unaltered or partially deprotected species, demonstrating effective shielding from first-pass metabolism. We conclude that prodrugs based on the N-monosubstituted carbamate ester bond have the appropriate stability profile for the systemic delivery of phenolic compounds. äAmino Acid Carbamates As Prodrugs Of Resveratrol (epmc).pdf DeepDyve Pubget Overpricing