Hydroxamic acid and fluorinated derivatives of valproic acid: Anticonvulsant activity, neurotoxicity and teratogenicity

2008 ◽  
Vol 30 (5) ◽  
pp. 390-394 ◽  
Author(s):  
Ute Gravemann ◽  
Jutta Volland ◽  
Heinz Nau
Author(s):  
J. Bruni ◽  
E.J. Hammond ◽  
B.J. Wilder

SUMMARY:The anticonvulsant activity of the ethyl esters of the major valproic acid metabolites was assessed against minimal pentylenetetrazol seizures in adult male ICR mice. The ethyl ester 3-hydroxy-propylpentanoic acid was found to possess significant anticonvulsant activity.


2009 ◽  
Vol 52 (22) ◽  
pp. 7236-7248 ◽  
Author(s):  
Dan Kaufmann ◽  
Meir Bialer ◽  
Jakob Avi Shimshoni ◽  
Marshall Devor ◽  
Boris Yagen

2012 ◽  
Vol 10 (2) ◽  
pp. 173-182 ◽  
Author(s):  
Jolanta Obniska ◽  
Iwona Chlebek ◽  
Krzysztof Kaminski ◽  
Andrzej J.Bojarski ◽  
Grzegorz Satala

2014 ◽  
Vol 14 (7) ◽  
pp. 984-993 ◽  
Author(s):  
Gabriela Luna-Palencia ◽  
Federico Martinez-Ramos ◽  
Ismael Vasquez-Moctezuma ◽  
Manuel Fragoso-Vazquez ◽  
Jessica Mendieta-Wejebe ◽  
...  

2017 ◽  
Vol 95 ◽  
pp. 25-30 ◽  
Author(s):  
Wafa Ben Cherif Khedhaier ◽  
Ichrak Dridi ◽  
Karim Aouam ◽  
Mossadok Ben-Attia ◽  
Alain Reinberg ◽  
...  

Pharmacia ◽  
2019 ◽  
Vol 66 (3) ◽  
pp. 141-146
Author(s):  
Hanna Severina ◽  
Olga O. Skupa ◽  
Natalya I. Voloshchuk ◽  
Marharyta M. Suleiman ◽  
Victoriya A. Georgiyants

The alkylation of 6-methyl-2-thioxo-2,3-dihydro-1H-pyrimidine-4-one phenacyl bromides under different conditions was investigated. It was found that during the reaction in the medium of DMF/K2CO3 a mixture of 2-(2-aryl-2-oxoethyl)thio-6-methyl-pyrimidine-4(3H)-one and 3-hydroxy-3-aryl-7-methyl-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-5-one was formed. The holding of the resulting mixture in the concentrated sulphuric acid leads to the formation of cyclization products - derivatives of 3-aryl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one with high yields. Individual S-alkylated derivatives – 2-(2-aryl-2-oxoethyl)thio-6-methyl-pyrimidine-4(3H)-one - were obtained by reacting in methanol in the presence of sodium methoxide. Pharmacological screening of synthesized compounds for anticonvulsant activity on the model of pentylenetetrazole seizures in rats was carried out and some regularity “structure-activity” was established.


2006 ◽  
Vol 59 (4) ◽  
pp. 283 ◽  
Author(s):  
Wamuyu Owotoki ◽  
Detlef Geffken ◽  
Thomas Kurz

Analogues of the antibiotic SF-2312 with a 3-substituted 1-hydroxypyrrolidine moiety have been prepared from 1-benzyloxy-3-bromopyrrolidin-2,5-dione (1) through Michaelis–Arbusov reaction with various trialkyl phosphites and subsequent alkylation of ring position 3. Cleavage of phosphonic esters 3 by TMSBr afforded the corresponding phosphonic acids 7, which were treated with ethanolamine to give the monosalts 8. Finally, hydrogenolysis furnished 1-hydroxypyrrolidin-2,5-diones 9.


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