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

Recent studies have demonstrated that functionalized alpha,alpha-diamino acids (1) display excellent activity when evaluated in the maximal electroshock seizure (MES) test in mice. The synthesis and pharmacological evaluation of 14 select analogues within this series of compounds are detailed. Inclu...

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Bibliographic Details
Published inJournal of pharmaceutical sciences Vol. 83; no. 5; pp. 689 - 691
Main Authors KOHN, H, SAWHNEY, KN, ROBERTSON, DW, LEANDER, JD
Format Journal Article
LanguageEnglish
Published WASHINGTON AMER PHARMACEUTICAL ASSN 01.05.1994
Subjects
Amino Acids, Diamino - chemical synthesis
Amino Acids, Diamino - pharmacology
Animals
Anticonvulsants - chemical synthesis
Anticonvulsants - pharmacology
Chemistry
Chemistry, Medicinal
Chemistry, Multidisciplinary
Dipeptides - chemical synthesis
Dipeptides - pharmacology
Life Sciences & Biomedicine
Male
Mice
Mice, Inbred Strains
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
Stereoisomerism
BENZOTRIAZOLE-ASSISTED SYNTHESIS
SERIES
AMINO-ACIDS
ANTIEPILEPTIC DRUG DEVELOPMENT
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Summary:Recent studies have demonstrated that functionalized alpha,alpha-diamino acids (1) display excellent activity when evaluated in the maximal electroshock seizure (MES) test in mice. The synthesis and pharmacological evaluation of 14 select analogues within this series of compounds are detailed. Included in this survey were 10 N-acyl derivatives in which the basic C(alpha) N-group in 1 was replaced by a neutral N-substituent and four dipeptides where the amino acid fusion point was the alpha-carbon site. N-Acylation of 1 led to decreased anticonvulsant activity. The importance of these findings in relation to the requirements of the C(alpha) substituent for anticonvulsant activity in 1 are briefly discussed.
ISSN:0022-3549
DOI:10.1002/jps.2600830519