Journal of medicinal chemistry

Design and evaluation of affinity labels of functionalized amino acid anticonvulsants

A LeTiran, JP Stables, H Kohn

Index: LeTiran, Arnaud; Stables, James P.; Kohn, Harold Journal of Medicinal Chemistry, 2002 , vol. 45, # 21 p. 4762 - 4773

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Citation Number: 29

Abstract

Studies have shown that functionalized amino acids (FAA) exhibit outstanding activity in the maximal electroshock-induced seizure (MES) test in rodents. Affinity labels patterned in part after the potent antiepileptic (R)-N-benzyl-2-acetamido-3-methoxypropionamide ((R)-2) have been prepared as mechanistic probes to learn the pharmacological basis for FAA function. The chemical reactivity of the affinity labels with nucleophiles was assessed, and ...