Bioorganic & medicinal chemistry letters

N, N′-Dialkylaminoalkylcarbonyl (DAAC) prodrugs and aminoalkylcarbonyl (AAC) prodrugs of 4-hydroxyacetanilide and naltrexone with improved skin permeation …

H Devarajan-Ketha, KB Sloan

Index: Devarajan-Ketha; Sloan Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 13 p. 4078 - 4082

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Citation Number: 5

Abstract

Abstract N, N′-Dialkylaminoalkylcarbonyl (DAAC) and aminoalkylcarbonyl (AAC) prodrugs of phenolic drugs acetaminophen (APAP) and naltrexone (NTX) are reported. The effects of incorporation of a basic amine group into the promoiety of an acyl prodrug of a phenolic drug on its skin permeation properties are also presented. DAAC-APAP prodrugs were synthesized via a three-step procedure starting with haloalkylcarbonyl esters which were ...