Synthesis of 2-piperidinecarboxylic acid derivatives as potential anticonvulsants

B Ho, PM Venkatarangan, SF Cruse, CN Hinko…

Index: Ho, Bin; Venkatarangan, Prabha M.; Cruse, Sharon F.; Hinko, Christine N.; Andersen, Peter H.; Crider, Albert M.; Adloo, Ahmad A.; Roane, David S.; Stables, James P. European Journal of Medicinal Chemistry, 1998 , vol. 33, # 1 p. 23 - 31

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Citation Number: 37

Abstract

A variety of 2-piperidinecarboxamides were synthesized and evaluated for anticonvulsant activity using the MES and sc PTZ tests in mice and rats. Neurotoxicity was determined by the rotorod test. Several N-(benzyl)-2-piperidinecarboxamides exhibited potent MES activity in mice [2-CF314, ED50= 29 mg/kg; 3-F 16, ED50= 31 mg/kg; and 3-CF317, ED50= 24 mg/kg]. The most active compounds in the MES test in mice were the 2, 6-dimethylanilides ...