Document Detail

Synthesis and characterization of aminoacidic pro-drugs of valproic acid.
MedLine Citation:
PMID:  9879567     Owner:  NLM     Status:  MEDLINE    
Some new derivatives of valproic acid (1) have been synthesized by condensation reaction of L-phenylalanine ethyl ester (2), L-tryptophan methyl ester (3), L-leucine methyl ester (4), L-methionine methyl ester (5) or L-histidine methyl ester (6) with 1 in the presence of dicyclohexylcarbodiimide (DCC). The reaction afforded in good yield prodrugs containing an amino acidic moiety. The structure of the new compounds was determined with the aid of spectroscopic and analytical data. To evaluate the stability following p.o., administration, the synthesized molecules were tested for gastro-intestinal hydrolysis. No significant general acid-base hydrolysis for the peptide bond was observed. The molecules offer a potentially useful mean to obtain highly selective drug release to the brain.
L I Giannola; L Lamartina; V de Caro
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Die Pharmazie     Volume:  53     ISSN:  0031-7144     ISO Abbreviation:  Pharmazie     Publication Date:  1998 Dec 
Date Detail:
Created Date:  1999-04-01     Completed Date:  1999-04-01     Revised Date:  2007-01-29    
Medline Journal Info:
Nlm Unique ID:  9800766     Medline TA:  Pharmazie     Country:  GERMANY    
Other Details:
Languages:  eng     Pagination:  829-34     Citation Subset:  IM    
Dipartimento di Chimica e Technologie Farmaceutiche, Università di Palermo, Italy.
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MeSH Terms
Amino Acids / chemistry*
Anticonvulsants / chemical synthesis*,  pharmacokinetics
Biological Availability
Digestive System / metabolism
Magnetic Resonance Spectroscopy
Prodrugs / chemical synthesis*,  pharmacokinetics
Valproic Acid / chemical synthesis*,  pharmacokinetics
Reg. No./Substance:
0/Amino Acids; 0/Anticonvulsants; 0/Prodrugs; 99-66-1/Valproic Acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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