ChemInform Abstract: PARA‐SUBSTITUTED N‐ACETYL‐L(S)‐ AND ‐D(R)‐α‐AMINO‐N‐PHENYLGLUTARIMIDES. A STRUCTURE‐ACTIVITY STUDY OF SUBSTITUENT EFFECTS ON STEREOSELECTIVE ANTICONVULSANT ACTIVITY

Witiak, Donald T.; Cook, Wayne L.; Gupta, T. K.; Gerald, Michael C.

doi:10.1002/chin.197716157

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“…Based on these estimates, it was concluded that the 6-amino-1,4-oxazepane-3,5-dione derivatives are anticonvulsant compounds enough to be recommended for new anticonvulsant drug candidates. Witak., et al 1972.…”

Section: Resultsmentioning

confidence: 98%

Synthesis and anticonvulsant evaluation of 6-amino-1,4-oxazepane-3,5-dione derivatives

Sharma

Park

2008

Arch. Pharm. Res.

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The N-Acyl-alpha-aminosuccinimides and N-Acyl-alpha-aminoglutarimides were reported to exhibit moderate anticonvulsant activities. These compounds were 5-membered or 6-membered alpha-amino cyclic imides and have N-CO-C-N moiety in their structures. Based on these structural characteristics, a series of 6-amino-1,4-oxazepine-3,5-dione derivatives 1, having a heterocyclic 7-memberd alpha-amino cyclic imide and N-CO-C-N moiety in their structures were designed and synthesized. These syntheses were in view to develop novel anticonvulsant compounds. The 6-amino-1, 4-oxazepine-3,5-dione derivatives were prepared from (S)-N-Cbz-serine by usual synthetic procedures and their anticonvulsant activities were examined by the MES and PTZ tests. The N-H (1a), N-methyl (1b), and N-n-butyl (1e) derivatives showed moderate anticonvulsant activities in the MES test. In the case of PTZ test, all the tested compounds except N-n-propyl compound(1c) also showed moderate anticonvulsant activities. Moreover, N-H (1a), N-methyl (1b), and N-n-butyl (1e) derivatives showed anticonvulsant activities in both the MES and PTZ test. From these studies, it was concluded that the 6-amino-1,4-oxazepane-3,5-dione derivatives were novel compounds enough to be recommended as new anticonvulsants.

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Section: Resultsmentioning

confidence: 98%

Synthesis and anticonvulsant evaluation of 6-amino-1,4-oxazepane-3,5-dione derivatives

Sharma

Park

2008

Arch. Pharm. Res.

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ChemInform Abstract: PARA‐SUBSTITUTED N‐ACETYL‐L(S)‐ AND ‐D(R)‐α‐AMINO‐N‐PHENYLGLUTARIMIDES. A STRUCTURE‐ACTIVITY STUDY OF SUBSTITUENT EFFECTS ON STEREOSELECTIVE ANTICONVULSANT ACTIVITY

Abstract: Früher beschriebene N‐Phenyl‐glutarimide (I) und (II) werden auf antikonvulsive Wirkung untersucht.

Cited by 1 publication

References 1 publication

Synthesis and anticonvulsant evaluation of 6-amino-1,4-oxazepane-3,5-dione derivatives

Synthesis and anticonvulsant evaluation of 6-amino-1,4-oxazepane-3,5-dione derivatives

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