56613-60-6Relevant articles and documents
Isolation, synthesis and photochemical properties of almazolone, a new indole alkaloid from a red alga of Senegal
Guella, Graziano,N'Diaye, Ibrahima,Fofana, Mouhamadou,Mancini, Ines
, p. 1165 - 1170 (2006)
An indole alkaloid bearing an oxazolone ring, christened almazolone, has been isolated from a new collection of Haraldiophyllum sp. from Dakar (Senegal), as an 88:12 mixture of (Z)/(E) stereoisomers. The relative ratio could be modified under controlled p
Solid phase synthesis of acylglycine human metabolites
Perez-Pineiro, Rolando,Dong, Ying Wei,Wishart, David S.
body text, p. 6706 - 6708 (2010/06/12)
Acylglycines represents a large and important class of human metabolites. They are often used in medicine to identify fatty acid oxidation disorders. A highly efficient solid phase synthesis approach to obtain these clinically important compounds is devel
N-(benzyloxycarbonyl)glycine esters and amides as new anticonvulsants
Geurts, Muriel,Poupaert, Jacques H.,Scriba, Gerhard K. E.,Lambert, Didier M.
, p. 24 - 30 (2007/10/03)
Glycine is a small neutral amino acid exhibiting weak anticonvulsant activities in vivo. Recently, studies have demonstrated that N- (benzyloxycarbonyl)glycine (1) antagonized seizures superior to glycine in addition to activity in the maximal electroshock (MES) test, a convulsive model where glycine is inactive. In the present study a series of ester and amide derivatives of 1 as well as esters of N-(3-phenylpropanoyl)glycine (5) have been prepared. The compounds were evaluated in the MES test as well as in several chemically induced seizure models. Among the derivatives investigated, N-(benzyloxycarbonyl)glycine benzylamide (16) was the most potent compound exhibiting an anticonvulsant activity in the MES test comparable to the drug phenytoin. Median effective doses (ED50) of 4.8 and 11.6 mg/kg were determined at 30 min and 3 h after ip administration, respectively. Compound 16 also effectively suppressed tonic seizures in different chemically induced models such as the strychnine, 3- mercaptopropionic acid, and pentylenetetrazole tests. Moreover, the compound studied here did not show acute neurotoxicity in the rotorod test up to a dose of 150 mg/kg. It is concluded that N-(benzyloxycarbonyl)glycine amides, especially 16, are potent anticonvulsant agents.