ANTICONVULSANT PROPERTIES OF N-SUBSTITUTED ALPHA,ALPHA-DIAMINO ACID-DERIVATIVES

Recent studies have demonstrated that functionalized alpha,alpha-diami no acids (1) display excellent activity when evaluated in the maximal electroshock seizure (MES) test in mice. The synthesis and pharmacolog ical evaluation of 14 select analogues within this series of compounds are detailed. Included in this survey were 10 N-acyl derivatives in w hich the basic C(alpha) N-group in 1 was replaced by a neutral N-subst ituent and four dipeptides where the amino acid fusion point was the a lpha-carbon site. N-Acylation of 1 led to decreased anticonvulsant act ivity. The importance of these findings in relation to the requirement s of the C(alpha) substituent for anticonvulsant activity in 1 are bri efly discussed.