| Design, synthesis, and anticonvulsant activity of new N-Mannich bases derived from spirosuccinimides and spirohydantoins. | |
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MedLine Citation:
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PMID: 20638856 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The synthesis and anticonvulsant properties of new N-Mannich bases of [7,8-f]benzo-2-aza-spiro[4.5]decane-1,3-diones (5a-h) and [7,8-f]benzo-1,3-diaza-spiro[4.5]decane-2,4-diones (7a-h) were described. Initial anticonvulsant screening was performed using intraperitoneal (ip) maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizures tests. The neurotoxicity was determined applying the rotarod test. The majority of compounds were effective in the MES or/and scPTZ screen. The quantitative studies showed that several molecules were more potent than phenytoin, used as reference drug. Selected derivatives were screened in the 6-Hz test and also assessed for potential activity against nerve agents using the Pilocarpine Induced Status Prevention model. To explain the possible mechanism of anticonvulsant action, for chosen active derivatives, their influence on voltage-dependent Na(+) channel were tested in vitro. |
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Authors:
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Jolanta Obniska; Hanna Byrtus; Krzysztof Kamiński; Maciej Pawłowski; Małgorzata Szczesio; Janina Karolak-Wojciechowska |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-06-30 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: 18 ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2010 Aug |
Date Detail:
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Created Date: 2010-08-09 Completed Date: 2010-12-06 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: England |
Other Details:
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Languages: eng Pagination: 6134-42 Citation Subset: IM |
Copyright Information:
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Copyright 2010 Elsevier Ltd. All rights reserved. |
Affiliation:
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Department of Medicinal Chemistry, Jagiellonian University, Medical College, Kraków, Poland. mfobnisk@cyf-kr.edu.pl |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anticonvulsants / chemical synthesis, chemistry*, therapeutic use* Electroshock Hydantoins / chemical synthesis, chemistry Male Mannich Bases / chemical synthesis, chemistry*, therapeutic use* Mice Pentylenetetrazole Rats Rats, Sprague-Dawley Seizures / chemically induced, drug therapy* Sodium Channels / metabolism Spiro Compounds / chemical synthesis, chemistry Succinimides / chemical synthesis, chemistry |
| Chemical | |
Reg. No./Substance:
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0/Anticonvulsants; 0/Hydantoins; 0/Mannich Bases; 0/Sodium Channels; 0/Spiro Compounds; 0/Succinimides; 123-56-8/succinimide; 54-95-5/Pentylenetetrazole |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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