Primary amino acid derivatives: substitution of the 4′-N′-benzylamide site in (R)-N′-benzyl 2-amino-3-methylbutanamide,(R)-N′-benzyl 2-amino-3, 3- …

AM King, C Salomé, E Salomé-Grosjean…

Index: King, Amber M.; Salome, Christophe; Dinsmore, Jason; Salome-Grosjean, Elise; De Ryck, Marc; Kaminski, Rafal; Valade, Anne; Kohn, Harold Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4815 - 4830

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Citation Number: 11

Abstract

Recently, we reported that select N′-benzyl 2-substituted 2-amino acetamides (primary amino acid derivatives (PAADs)) exhibited pronounced activities in established whole animal anticonvulsant (ie, maximal electroshock seizure (MES)) and neuropathic pain (ie, formalin) models. The anticonvulsant activities of C (2)-hydrocarbon N′-benzyl 2-amino acetamides (MES ED50= 13–21 mg/kg) exceeded those of phenobarbital (ED50= 22 mg/ ...