Nipecotic acid, prodrugs

A few of the phenyl esters of nipecotic acid were also examined for their anticonvulsant effects and found to be active. The most stable ester was also the most active, but more labile esters were also effective. Because nipecotic acid itself was not used for comparison, no conclusion can be derived regarding the pharmacological value of such prodrugs. 

C. Altomare, A. Carotti, S. Cellamare, M. Ferappi, R. Cagiano, G. Renna, QSAR Analysis of Chemical and Serum-Catalyzed Hydrolysis of Phenyl Ester Prodrugs of Nipecotic Acid , Int. J. Pharm. 1988, 48, 91 -102. 

Lipophilic prodrugs can also be derived from a carboxylic function, the most commonly used derivatives being carboxylic esters. Simple esters of aliphatic alcohols are attractive as they are cheap to prepare, chemically stable, and yield harmless hydrolysis products." Typical representatives of such prodrugs are tyrosine methyl ester," levodopa ethyl ester," nipecotic acid ethyl ester," enala-prilat ethyl ester," " " trandolapril," y-aminobutyric acid cetyl ester" " and methotrexate cetyl ester." ... 

S. Tanganelli, L. Perraro, P. Prasad, and A. Dalpiaz,/. Med. Chem., 45, 559 (2002). Design, Synthesis and Activity of Ascorbic Acid Prodrugs of Nipecotic, Kynurenic and Diclophe-namic Acids, Liable to Increase Neurotropic Activity. 

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