Anticonvulsant Profiles of Certain New 6-Aryl-9-substituted- 6,9-diazaspiro-[4.5]decane-8,10-diones and 1-Aryl-4-substituted- 1,4-diazaspiro[5.5]undecane-3,5-diones

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dc.contributor.author Aboul-Enein, Mohamed N.
dc.contributor.author El-Azzouny, Aida A.
dc.contributor.author Attia, Mohamed I.
dc.contributor.author Maklad, Yousreya A.
dc.contributor.author Aboutabl, Mona E.
dc.contributor.author Ragab, Fatma
dc.contributor.author Abd El-Hamid, Walaa H. A.
dc.date.accessioned 2017-09-13T14:25:15Z
dc.date.available 2017-09-13T14:25:15Z
dc.date.issued 2014-09-23
dc.identifier.citation Aboul-Enein, M. N., El-Azzouny, A. A., Attia, M. I., Maklad, Y. A., Aboutabl, M. E., Ragab, F., & Abd El-Hamid, W. H. (2014). Anticonvulsant Profiles of Certain New 6-Aryl-9-substituted- 6,9-diazaspiro-[4.5]decane-8,10-diones and 1-Aryl-4-substituted- 1,4-diazaspiro[5.5]undecane-3,5-diones. International Journal of Molecular Sciences. doi:10.3390/ijms150916911
dc.identifier.issn 14220067
dc.identifier.uri http://dspace.must.edu.eg/handle/123456789/255
dc.description.abstract Synthesis and anticonvulsant potential of certain new 6-aryl-9-substituted-6,9- diazaspiro[4.5]decane-8,10-diones (6a–l) and 1-aryl-4-substituted-1,4-diazaspiro[5.5] undecane-3,5-diones (6m–x) are reported. The intermediates 1-[(aryl)(cyanomethyl)amino] cycloalkanecarboxamides (3a–f) were prepared via adopting Strecker synthesis on the proper cycloalkanone followed by partial hydrolysis of the obtained nitrile functionality and subsequent N-cyanomethylation. Compounds 3a–f were subjected to complete nitrile hydrolysis to give the respective carboxylic acid derivatives 4a–f which were cyclized under mild conditions to give the spiro compounds 5a–f. Ultimately, compounds 5a–f were alkylated or aralkylated to give the target compounds 6a–i and 6m–u. On the other hand, compounds 6j–l and 6v–x were synthesized from the intermediates 5a–f through OPEN ACCESS alkylation, dehydration and finally tetrazole ring formation. Anticonvulsant screening of the target compounds 6a–x revealed that compound 6g showed an ED50 of 0.0043 mmol/kg in the scPTZ screen, being about 14 and 214 fold more potent than the reference drugs, Phenobarbital (ED50 = 0.06 mmol/kg) and Ethosuximide (ED50 = 0.92 mmol/kg), respectively. Compound 6e exhibited an ED50 of 0.019 mmol/kg, being about 1.8 fold more potent than that of the reference drug, Diphenylhydantoin (ED50 = 0.034 mmol/kg) in the MES screen. Interestingly, all the test compounds 6a–x did not show any minimal motor impairment at the maximum administered dose in the neurotoxicity screen. en_US
dc.language.iso en en_US
dc.publisher International Journal of Molecular Sciences en_US
dc.relation.ispartofseries International Journal of Molecular Sciences;
dc.subject cycloalkanones en_US
dc.subject Strecker synthesis en_US
dc.subject alkylation en_US
dc.subject spiro compounds en_US
dc.subject tetrazole en_US
dc.subject anticonvulsant en_US
dc.title Anticonvulsant Profiles of Certain New 6-Aryl-9-substituted- 6,9-diazaspiro-[4.5]decane-8,10-diones and 1-Aryl-4-substituted- 1,4-diazaspiro[5.5]undecane-3,5-diones en_US
dc.type Article en_US


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