- Glycine derivatives of imidazolones as potential ligands of glycine binding site of NMDA receptors. Part 1
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The series of glycine derivatives of diphenyl or (un)substituted arylidene imidazolones was designed and obtained as potential ligands of the glycine binding site of NMDA receptors. The compounds were evaluated in vitro for their affinity to the glycine b
- Kiec-Kononowicz, Katarzyna,Karolak-Wojciechowska, Janina,Handzlik, Jadwiga
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p. 381 - 388
(2007/10/03)
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- Synthesis and Anticonvulsant Activity of 2-Iminohydantoins
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Iminohydantoins selectively substituted at position C-5 and their 1-carbobenzoxy derivatives have been synthesized, and their anticonvulsant activity was evaluated in mice.In general, the more lipophilic 1-carbobenzoxy iminohydantoins were more potent than the unsubstituted counterparts.Evaluation of the individual enantiomers of the chiral iminohydantoins showed that the anticonvulsant activity resided primarily in the S isomers.In this study, (S)-(+)-1-carbobenzoxy-5-isobutyl-2-iminohydantoin (9a) was the most active member.This compound was not nearly as active as phenythoin against electrically induced convulsions, but was also active against pentylenetetrazole-induced seizures, suggesting a broader clinical potential.The closest analogue of phenytoin, viz., 5,5-diphenyl-2-iminohydantoin (1), failed to show any significant activity.Methylation on N-3 or the imino nitrogen of 1 also did not provide a compound with substantial activity. 2-Thiophenytoin was not active against electoshock seizures and showed only a weak activity against pentylenetetrazole.This study suggested that the structure-activity relationship of 2-iminohydantoins was quite different from that of 2-hydantoins.
- Kwon, Chul-Hoon,Iqbal, Muhammad Tahir,Wurpel, John N. D.
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p. 1845 - 1849
(2007/10/02)
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- SYNTHESIS OF SOME 5,5-DISUBSTITUTED 2-THIOHYDANTOIN DERIVATIVES
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Treatment of 5,5-diphenyl-2-thiohydantoin (2a) with allyl bromide in basic alcohol solution gave 5,5-diphenyl-2-allylthiohydantoin (3a) in 78.5percent yield, whose derivatives (3b), (3f), (4a-c), and (6) were also prepared in a similar fashion.
- Chiang, Hung-Cheh,Ko, Jin-Ren
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p. 529 - 530
(2007/10/02)
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