ChemInform Abstract: PUFEMIDE ‐ A NEW USSR ANTIEPILEPTIC DRUG

Mndzhoyan, O. L.; Avetisyan, S. A.; Akopyan, N. E.; Gerasimyan, D. A.; Dzhagatspanyan, I. A.; Pashinyan, S. A.

doi:10.1002/chin.198349197

Cited by 2 publications

(3 citation statements)

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“…The last example does not seem to be consistent with data obtained in (9), according to which imine linker joining the endocyclic N atom and aromatic moiety was essential for anticonvulsant activity. Also, the binding of two molecules of 1 by N-atoms through a benzene ring (14) gave a negative effect. Compounds 25 and 26, containing benzimidazolyl fragments are devoid at all of the activity in question, although information about the anticonvulsant activity of benzimidazole derivatives has been known (29,30).…”

Section: Discussionmentioning

confidence: 99%

“…However, when an additional an methyl group was introduced in position 3 of the same imides, the pattern of resulting activities was found to be dependent on some experimental seizure model. The most effective was the 1,3-dimethyl derivative of 3-p-isopropoxyphenylsuccinimide (14). To carry out the study of the structure-activity relationship, two molecules of 3-p-isopropoxyphenylsuccinimide were coupled by their N atoms directly (N-N-bond), and through linear alkylene chains (C 1 -C 10 ) (15).…”

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confidence: 99%

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Synthesis and Anticonvulsant Properties of Some N-Aryl and N-Arylaminomethyl Derivatives of 3-P-Isopropoxyphenylpyrrolidine-2,5-Dione

Kocharov¹,

Panosyan²,

Chmielewski³

et al. 2019

Acta Poloniae Pharmaceutica - Drug Research

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Anticonvulsant properties of newly synthesized compounds and potential antiepileptic drugs are usually assessed in screen tests in experimental animals. One of the most commonly used screen tests in mice is the maximal electroshock-induced seizure test that reflects tonic-clonic seizures in humans. A series of 3-p-isopropoxyphenylpyrrolidine-2,5-dione derivatives, including N-aryl and N-arylaminomethyl analogs, were characterized for their anticonvulsant properties in the maximal electroshock-induced seizure test in mice. Electroconvulsions (tonic-clonic seizures) were evoked in adult Albino Swiss mice by a current (sine-wave, 25 mA, 50 Hz, 500 V, 0.2 s stimulus duration) delivered via auricular electrodes. N-aryl derivatives did not show any anticonvulsant activity, whereas some representatives of N-arylaminomethyl derivatives, i.e. N-Mannich bases, exhibited a distinct protective action against maximal electroshock-induced (MES) convulsions in mice. Several N-arylaminomethyl derivatives of 3-p-isopropoxyphenylpyrrolidine-2,5-dione may become in future new antiepileptic drugs, or they could serve as valuable supporting materials for obtaining new derivatives with stronger anticonvulsant activities than their maternal compounds.

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Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

Synthesis and Anticonvulsant Properties of Some N-Aryl and N-Arylaminomethyl Derivatives of 3-P-Isopropoxyphenylpyrrolidine-2,5-Dione

Kocharov¹,

Panosyan²,

Chmielewski³

et al. 2019

Acta Poloniae Pharmaceutica - Drug Research

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“…Recently, a significant anticonvulsant activity of 3-(4-isopropoxyphenyl)-pyrrolidine-2,5-dione (3-p-isopropoxyphenylsuccinimide) was observed and this compound was introduced into medical practice in the former Soviet Union [10] under the trade name 'Pufemid'. In view of all the above, it was considered expedient to search for the influence of additional chemical modification of the molecule of 3-p-isopropoxyphenylsuccinimide on its biological properties, namely, on expected changes in the anticonvulsant activity.…”

Section: Introductionmentioning

confidence: 99%