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Synthesis and investigation of anti-inflammatory and anticonvulsant activities of novel coumarin-diacylated hydrazide derivatives

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dc.contributor.authorÇAM, MUHAMMET EMİN
dc.contributor.authorsTapanyigit, Ozan; Demirkol, Onur; Guler, Ece; Ersatir, Mehmet; Cam, Muhammet Emin; Giray, Elife Sultan
dc.date.accessioned2022-03-14T09:20:20Z
dc.date.available2022-03-14T09:20:20Z
dc.date.issued2020-12
dc.description.abstractA number of novel coumarin derivatives synthesized by the reaction of 3-carbonyl chloride coumarin with some substituted aryl acid hydrazides to investigate their anti-inflammatory and anticonvulsant activities. Carrageenan (0.1 ml of 1%, w/v) was injected subplantarly in the right paw of rats to induce an acute model of inflammation. Anti-inflammatory efficacy was evaluated for 5 hours at 3 different dosages 5, 10, 25 mg/kg. After that, the changes in the level of paw edema volumes and percentage inhibition of all groups were observed and the most effective coumarin derivative was found as N'-(2-hyroxybenzoyl)-2-oxo-2H-chromene-3-carbohydrazide. In addition, N'-(2-oxo-2H-chromene-3-carbonyl)nicotinohydrazide, (E)-N'-(3-(4-hydroxyphenyl)acryloyl)-2-oxo-2H-chromene-3-carbohydrazide, and N'-(5-amino-2-hydroxybenzoyl)-2-oxo-2H-chromone-3carbohydrazide showed their anti-inflammatory effects in a dose-dependent manner. On the other hand, pentylenetetrazole (PTZ, 80 mg/kg, i.p.)-induced seizure model was used to investigate the anticonvulsant activities of six newly synthesized coumarin derivatives in mice. Hybrid compound of salicylic acid hydrazide and 3-carbonyl chloride coumarin (8d) was found the most promising anticonvulsant agent among all treatment groups according to the onset of seizure and survival rate. Moreover, (E)-N'-cinnamoyl-2-oxo-2H-chromene-3-carbohyrazide (8b) and (E)-N'-(3-(4-hyroxy phenyl)acryloyl)-2-oxo-2H-chromene-3-carbohydrazide (8c) has potential anticonvulsant efficiency in low doses (30 mg/kg). The anticonvulsant effect of these coumarin derivatives may be through enhanced GABA-mediated inhibition in the brain. (C) 2020 Published by Elsevier B.V. on behalf of King Saud University.
dc.identifier.doi10.1016/j.arabjc.2020.10.034
dc.identifier.eissn1878-5379
dc.identifier.issn1878-5352
dc.identifier.urihttps://hdl.handle.net/11424/242985
dc.identifier.wosWOS:000600552400045
dc.language.isoeng
dc.publisherELSEVIER
dc.relation.ispartofARABIAN JOURNAL OF CHEMISTRY
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectAnti-inflammatory activity
dc.subjectAnticonvulsant activity
dc.subjectCoumarin-diacylated hydrazide
dc.subjectPentylenetetrazole-induced seizures
dc.subjectCarrageenan-induced paw edema
dc.subjectN,N'-DIACYLHYDRAZINE DERIVATIVES
dc.subjectBIOLOGICAL-ACTIVITIES
dc.subjectACID-DERIVATIVES
dc.subjectSEIZURE ACTIVITY
dc.subjectANTIOXIDANT
dc.subjectEPILEPSY
dc.subjectEXTRACT
dc.subjectMETHYL
dc.subjectBIOACTIVITY
dc.titleSynthesis and investigation of anti-inflammatory and anticonvulsant activities of novel coumarin-diacylated hydrazide derivatives
dc.typearticle
dspace.entity.typePublication
local.avesis.ida01eb685-dd81-4861-a7c0-24af7f6f4b5d
local.import.packageSS16
local.indexed.atWOS
local.indexed.atSCOPUS
local.journal.numberofpages13
local.journal.quartileQ2
oaire.citation.endPage9117
oaire.citation.issue12
oaire.citation.startPage9105
oaire.citation.titleARABIAN JOURNAL OF CHEMISTRY
oaire.citation.volume13
relation.isAuthorOfPublication96f1bd4e-81dc-4c34-bbf2-e15edc6f01b3
relation.isAuthorOfPublication.latestForDiscovery96f1bd4e-81dc-4c34-bbf2-e15edc6f01b3

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