Synthesis and Anticonvulsant Activity of Aminoacid-derived sulfamides

GAVERNET LUCIANA; ELVIRA JUAN E.; SAMAJA GISELA; PASTORE VALENTINA; SELLA CRAVERO MARIANA; ENRIQUE ANDREA; ESTIU GUILLERMINA; BRUNO BLANCH LUIS E.

Trieste, italia

Conferencia; 2nd Conference on Drug Development for the Third Word: From computacional Biology to Experimental Approaches; 2009

Amino acids and their derivatives have been investigated for their anticonvulsant action, and some of them were found to be potent AEDs.9 Several second-generation drugs, as well as drugs in development, have this functionality in their structures. We report herein the synthesis and anticonvulsant activity of a set of amino acid-derived sulfamides. In some compounds, the sulfamide is a nonhydrolyzable linker of two amino ester groups (compounds 1-3, Figure 1), whereas in other structures it connects a lipophilic (alkyl/aryl) group with amino esters (10-12 and 14-16, Figure 1). The most promising compounds are 10, 11, and 16, and for them the median effective dose ED50 values for the anticonvulsant activity in the MES test,10 were determined.