Synthesis, Molecular Docking Studies, and Anticonvulsant Evaluation of Novel bis‐Phenylhydrazones against Chemically induced Seizures in Mice
A series of novel bis‐phenylhydrazones were synthesized by the condensation of dialdehydes with phenylhydrazine to evaluate them for their anticonvulsant activity. Efficacy of newly synthesized compounds against pentylenetetrazole (PTZ)‐induced, strychnine‐induced, and picrotoxin‐induced convulsions...
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Veröffentlicht in: | Journal of the Chinese Chemical Society (Taipei) 2017-08, Vol.64 (8), p.940-952 |
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description | A series of novel bis‐phenylhydrazones were synthesized by the condensation of dialdehydes with phenylhydrazine to evaluate them for their anticonvulsant activity. Efficacy of newly synthesized compounds against pentylenetetrazole (PTZ)‐induced, strychnine‐induced, and picrotoxin‐induced convulsions was tested after administration of these compounds to albino mice via the oral route. All the five tested compounds showed anticonvulsant activity against strychnine‐induced and picrotoxin‐induced convulsions in a dose‐dependent manner. However, the effect was more significant against PTZ‐induced convulsions. Behavioral pattern studies on mice suggested that these compounds are less neurotoxic compared to phenytoin. Molecular docking studies were carried out to correlate the experimental and theoretical results. It was concluded that these compounds exerted their anticonvulsant effect through the modification of the function of GABA receptor‐mediated chloride channels. Molecular docking studies revealed a good correlation, which indicated that in silico studies could provide an alternate tool for the identification and design of more potent anticonvulsant agents.
A series of novel bis‐phenylhydrazones was synthesized. Anticonvulsant behavior of newly synthesized compounds were tested after administration of these compounds to albino mice via oral route. All the five test compounds showed anticonvulsant activity. Molecular docking studies were carried out to correlate experimental and theoretical results. These studies revealed a good correlation between experimental and docking results. |
doi_str_mv | 10.1002/jccs.201700038 |
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A series of novel bis‐phenylhydrazones was synthesized. Anticonvulsant behavior of newly synthesized compounds were tested after administration of these compounds to albino mice via oral route. All the five test compounds showed anticonvulsant activity. Molecular docking studies were carried out to correlate experimental and theoretical results. These studies revealed a good correlation between experimental and docking results.</description><identifier>ISSN: 0009-4536</identifier><identifier>EISSN: 2192-6549</identifier><identifier>DOI: 10.1002/jccs.201700038</identifier><language>eng</language><publisher>Weinheim: Wiley‐VCH Verlag GmbH & Co. KGaA</publisher><subject>Anticonvulsant ; Anticonvulsants ; bis‐Phenylhydrazones ; Chemical synthesis ; Convulsions ; Correlation analysis ; Mice ; Molecular docking ; Molecular operating environment (MOE) ; Seizures ; Strychnine</subject><ispartof>Journal of the Chinese Chemical Society (Taipei), 2017-08, Vol.64 (8), p.940-952</ispartof><rights>2017 The Chemical Society Located in Taipei & Wiley‐VCH Verlag GmbH & Co. KGaA, Weinheim</rights><rights>2017 The Chemical Society Located in Taipei & Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3158-d8108ab68b10066c7192526d74e00cfede10be6982fbc5f98e4e20345e5ab88b3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fjccs.201700038$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjccs.201700038$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1417,27923,27924,45573,45574</link.rule.ids></links><search><creatorcontrib>Siddiqi, Humaira Masood</creatorcontrib><creatorcontrib>Tabasum, Aneela</creatorcontrib><creatorcontrib>Qasim, Sumera</creatorcontrib><creatorcontrib>Akhtar, Muhammad Shoaib</creatorcontrib><creatorcontrib>Kalsoom, Saima</creatorcontrib><creatorcontrib>Ansari, Farzana Latif</creatorcontrib><title>Synthesis, Molecular Docking Studies, and Anticonvulsant Evaluation of Novel bis‐Phenylhydrazones against Chemically induced Seizures in Mice</title><title>Journal of the Chinese Chemical Society (Taipei)</title><description>A series of novel bis‐phenylhydrazones were synthesized by the condensation of dialdehydes with phenylhydrazine to evaluate them for their anticonvulsant activity. Efficacy of newly synthesized compounds against pentylenetetrazole (PTZ)‐induced, strychnine‐induced, and picrotoxin‐induced convulsions was tested after administration of these compounds to albino mice via the oral route. All the five tested compounds showed anticonvulsant activity against strychnine‐induced and picrotoxin‐induced convulsions in a dose‐dependent manner. However, the effect was more significant against PTZ‐induced convulsions. Behavioral pattern studies on mice suggested that these compounds are less neurotoxic compared to phenytoin. Molecular docking studies were carried out to correlate the experimental and theoretical results. It was concluded that these compounds exerted their anticonvulsant effect through the modification of the function of GABA receptor‐mediated chloride channels. Molecular docking studies revealed a good correlation, which indicated that in silico studies could provide an alternate tool for the identification and design of more potent anticonvulsant agents.
A series of novel bis‐phenylhydrazones was synthesized. Anticonvulsant behavior of newly synthesized compounds were tested after administration of these compounds to albino mice via oral route. All the five test compounds showed anticonvulsant activity. Molecular docking studies were carried out to correlate experimental and theoretical results. These studies revealed a good correlation between experimental and docking results.</description><subject>Anticonvulsant</subject><subject>Anticonvulsants</subject><subject>bis‐Phenylhydrazones</subject><subject>Chemical synthesis</subject><subject>Convulsions</subject><subject>Correlation analysis</subject><subject>Mice</subject><subject>Molecular docking</subject><subject>Molecular operating environment (MOE)</subject><subject>Seizures</subject><subject>Strychnine</subject><issn>0009-4536</issn><issn>2192-6549</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid/><recordid>eNo9kM1OwzAQhC0EEqVw5WyJKymOnaT2sQrlTy0gFc6R42xaF9cucVKUnngDeEaehFRFnFa782lWMwidh2QQEkKvlkr5ASXhkBDC-AHq0VDQIIkjcYh63U0EUcySY3Ti_ZKQiNFY9NDXrLX1Arz2l3jqDKjGyApfO_Wm7RzP6qbQ0EnSFnhka62c3TTGS1vj8UaaRtbaWexK_Og2YHCu_c_n9_MCbGsWbVHJrbPgsZxLbX2N0wWstJLGtFjbolFQ4BnobVN1jLZ4qhWcoqNSGg9nf7OPXm_GL-ldMHm6vU9Hk0CxMOZBwUPCZZ7wvIueJGrYRY1pUgwjIESVUEBIckgEp2Wu4lJwiIASFsUQy5zznPXRxd53Xbn3BnydLV1T2e5l1lkJJggTtKPEnvrQBtpsXemVrNosJNmu8WzXePbfePaQprP_jf0CN1p66w</recordid><startdate>201708</startdate><enddate>201708</enddate><creator>Siddiqi, Humaira Masood</creator><creator>Tabasum, Aneela</creator><creator>Qasim, Sumera</creator><creator>Akhtar, Muhammad Shoaib</creator><creator>Kalsoom, Saima</creator><creator>Ansari, Farzana Latif</creator><general>Wiley‐VCH Verlag GmbH & Co. KGaA</general><general>Wiley Subscription Services, Inc</general><scope/></search><sort><creationdate>201708</creationdate><title>Synthesis, Molecular Docking Studies, and Anticonvulsant Evaluation of Novel bis‐Phenylhydrazones against Chemically induced Seizures in Mice</title><author>Siddiqi, Humaira Masood ; Tabasum, Aneela ; Qasim, Sumera ; Akhtar, Muhammad Shoaib ; Kalsoom, Saima ; Ansari, Farzana Latif</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3158-d8108ab68b10066c7192526d74e00cfede10be6982fbc5f98e4e20345e5ab88b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Anticonvulsant</topic><topic>Anticonvulsants</topic><topic>bis‐Phenylhydrazones</topic><topic>Chemical synthesis</topic><topic>Convulsions</topic><topic>Correlation analysis</topic><topic>Mice</topic><topic>Molecular docking</topic><topic>Molecular operating environment (MOE)</topic><topic>Seizures</topic><topic>Strychnine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Siddiqi, Humaira Masood</creatorcontrib><creatorcontrib>Tabasum, Aneela</creatorcontrib><creatorcontrib>Qasim, Sumera</creatorcontrib><creatorcontrib>Akhtar, Muhammad Shoaib</creatorcontrib><creatorcontrib>Kalsoom, Saima</creatorcontrib><creatorcontrib>Ansari, Farzana Latif</creatorcontrib><jtitle>Journal of the Chinese Chemical Society (Taipei)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Siddiqi, Humaira Masood</au><au>Tabasum, Aneela</au><au>Qasim, Sumera</au><au>Akhtar, Muhammad Shoaib</au><au>Kalsoom, Saima</au><au>Ansari, Farzana Latif</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis, Molecular Docking Studies, and Anticonvulsant Evaluation of Novel bis‐Phenylhydrazones against Chemically induced Seizures in Mice</atitle><jtitle>Journal of the Chinese Chemical Society (Taipei)</jtitle><date>2017-08</date><risdate>2017</risdate><volume>64</volume><issue>8</issue><spage>940</spage><epage>952</epage><pages>940-952</pages><issn>0009-4536</issn><eissn>2192-6549</eissn><abstract>A series of novel bis‐phenylhydrazones were synthesized by the condensation of dialdehydes with phenylhydrazine to evaluate them for their anticonvulsant activity. Efficacy of newly synthesized compounds against pentylenetetrazole (PTZ)‐induced, strychnine‐induced, and picrotoxin‐induced convulsions was tested after administration of these compounds to albino mice via the oral route. All the five tested compounds showed anticonvulsant activity against strychnine‐induced and picrotoxin‐induced convulsions in a dose‐dependent manner. However, the effect was more significant against PTZ‐induced convulsions. Behavioral pattern studies on mice suggested that these compounds are less neurotoxic compared to phenytoin. Molecular docking studies were carried out to correlate the experimental and theoretical results. It was concluded that these compounds exerted their anticonvulsant effect through the modification of the function of GABA receptor‐mediated chloride channels. Molecular docking studies revealed a good correlation, which indicated that in silico studies could provide an alternate tool for the identification and design of more potent anticonvulsant agents.
A series of novel bis‐phenylhydrazones was synthesized. Anticonvulsant behavior of newly synthesized compounds were tested after administration of these compounds to albino mice via oral route. All the five test compounds showed anticonvulsant activity. Molecular docking studies were carried out to correlate experimental and theoretical results. These studies revealed a good correlation between experimental and docking results.</abstract><cop>Weinheim</cop><pub>Wiley‐VCH Verlag GmbH & Co. KGaA</pub><doi>10.1002/jccs.201700038</doi><tpages>13</tpages></addata></record> |
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subjects | Anticonvulsant Anticonvulsants bis‐Phenylhydrazones Chemical synthesis Convulsions Correlation analysis Mice Molecular docking Molecular operating environment (MOE) Seizures Strychnine |
title | Synthesis, Molecular Docking Studies, and Anticonvulsant Evaluation of Novel bis‐Phenylhydrazones against Chemically induced Seizures in Mice |
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