5241-66-7Relevant articles and documents
Primary amino acid derivatives: Compounds with anticonvulsant and neuropathic pain protection activities
King, Amber M.,Salomé, Christophe,Dinsmore, Jason,Salomé-Grosjean, Elise,De Ryck, Marc,Kaminski, Rafal,Valade, Anne,Kohn, Harold
supporting information; experimental part, p. 4815 - 4830 (2011/10/01)
Pharmacological management remains the primary method to treat epilepsy and neuropathic pain. We have advanced a novel class of anticonvulsants termed functionalized amino acids (FAAs). In this study, we examine FAA derivatives from which the terminal acetyl moiety was removed and termed these compounds primary amino acid derivatives (PAADs). Twenty-seven PAADs were prepared; the central C(2) R-substituent was varied, including C(2) stereochemistry, and the compounds were tested in rodent models of seizures and neuropathic pain. C(2)-Hydrocarbon N-benzylamide PAADs were potent anticonvulsants and excellent anticonvulsant activity (mice, ip; rat, po) was observed for C(2) R-substituted PAADs in which the R group was ethyl, isopropyl, or tert-butyl, and the C(2) stereochemistry conformed to the d-amino acid configuration ((R)-stereoisomer). These values surpassed the activities of several clinical antiepileptic drugs. The C(2) (R)-ethyl and C(2) (R)-isopropyl PAADs also displayed excellent activities in the mouse (ip) formalin neuropathic pain model. Significantly, unlike the FAA structure-activity relationship, PAAD anticonvulsant activity increased upon substitution of a methylene unit for a heteroatom in the R-substituent that was one atom removed from the C(2) site, suggesting that these PAADs function by a different pathway than FAAs.
[3R]-3-amino-1-hydroxy pyrrolidin-2-one and its use as a neuroprotective agent
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, (2008/06/13)
The present invention provides R(+)-3-amino-1-hydroxypyrrolidin-2-one of formula I: STR1 or pharmaceutically acceptable acid addition salt thereof, which compound is useful as an anticonvulsant agent and in the treatment and/or prevention of neurodegenerative disorders.
FORMATION CONSTANTS OF SILVER(I) COMPLEXES OF SOME SULPHUR-CONTAINING DIPEPTIDES AND VALYLVALINE
Lyons, Anthony Q.,Pettit, Leslie D.
, p. 2305 - 2308 (2007/10/02)
Formation constants at 25 deg C and l = 0.10 mol dm-3 (KNO3) have been determined for the complexes of AgI with a range of nine dipeptides which incorporate side-chains containing one (glycylmethionine and methionylglycine) or two sulphur donor atoms.In the latter case dipeptides formed from amino acids of the same and of different chiralities were studied (e.g.L-methionyl-L-methionine and L-methionyl-D-methionine).The results are compared with those for valylvaline.Values for the formation constants are interpreted in terms of the preferred conformations of the dipeptides, and the tendency for AgI to bond to S-donor atoms or to adopt linear co-ordination through the formation of dimeric complexes.
