Synthesis and in vivo evaluation of non-hepatotoxic acetaminophen analogs

…, C Sunkel, J Alvarez-Builla, NG Bazan

Index: Vaccarino, Anthony L.; Paul, Dennis; Mukherjee, Pranab K.; Rodriguez de Turco, Elena B.; Marcheselli, Victor L.; Xu, Liang; Trudell, Mark L.; Minguez; Matia; Sunkel, Carlos; Alvarez-Builla, Julio; Bazan, Nicolas G. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 5 p. 2206 - 2215

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Citation Number: 28

Abstract

A series of acetaminophen (APAP) analogs, 2-(1, 1-dioxido-3-oxo-1, 2-benzisothiazol-2 (3H)- yl)-N-(4-hydroxyphenyl) alkanecarboxamides, bearing a heterocyclic moiety linked to the p- acylaminophenol fragment, were prepared in a general project to develop APAP analogs with modulated pharmacokinetic profiles. Unexpectedly, the products described maintained the in vivo analgesic profile, while the characteristic hepatotoxicity of APAP was ...