Synthesis and anticonvulsant activity of some 4-nitro-N-phenylbenzamides

Bailleux, V.; Vallée, Louis; Nuyts, Jean-Pierre; Hamoir, G.; Poupaert, Jacques H.; Stables, J. P.; Vamecq, Jòseph

doi:10.1016/0223-5234(96)88254-7

Cited by 12 publications

(6 citation statements)

References 9 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…According top hase1of the anticonvulsants creening project(ASP),twoconvulsantt ests,maximale lectroshock( MES)and pentylenetetrazole (ScPTZ),a reused forprimary evaluation foranticonvulsantactivity and the rotarod test isu sed forprimary toxicity screening [28].The anticonvulsantactivity of the title compounds wasdetermined against MES seizuresduetothe reported datarevealing the anti-MES activity of anilide pharmacophore [9][10][13][14][15][16][17][18][19].The MES test isamodel forgeneralized tonic-clonicseizuresand represents the compoundspreventing seizurespreads [28].The activity dataof the title compoundsagainst MES seizuresinduced 0.5 and 4h afteradministration atasingle dose level of 100 mg/kg aresummarized in Table 4. Also,the primary neurologicaltoxicity of the compoundsdetermined byt he rotarod test ispresented in Table 4.…”

Section: 2anticonvulsantactivitymentioning

confidence: 99%

“…Inrecenty ears,one of the common strategiesfort he developmentof the newAEDsismolecularmodification of the knownd rugsormoleculesw ithanticonvulsant activity.Anilide,one of the pharmacophoresw ithanticonvulsantactivity against maximale lectroshockseizures(MES)wass tudied extensivelybyt he research groupsof Clarkand Vamecq [8][9][10][11][12][13][14][15][16].Ho etal. alsostudied anilide derivativesand reported N -(2,6-dimethylphenyl)piperidine-2-carboxamide ast he most active molecule [17].Inthe lightof thesestudies,anti-MES activity of anilide pharmacophorei sdepending on the substitution patternand the natureo fthe substituent on the N -phenylring.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Synthesis and anticonvulsant activity of some alkanamide derivatives

Tarikogullari

Fatma

Erol

et al. 2011

Arzneimittelforschung

View full text Add to dashboard Cite

A group of N-phenylacetamide, N-phenylpropanamide and N-benzylamide derivatives bearing 5-membered heterocyclic rings such as pyrazole, 1,2,4-triazole and imidazole rings at omega position were synthesized and their anticonvulsant activity was evaluated in the maximal electroshock test. The results indicated that the 1,2,4-triazole ring leads to superior activity than the pyrazole ring and inserting a CH2 group into the anilide structure leading to N-benzyl derivatives did not change the anticonvulsant activity, but caused a noticeable decrease in duration of action. The most active compound was 2-(1H-1,2,4-triazole-1-yl)-N-(2,6-dimethylphenyl)acetamide.

show abstract

Section: 2anticonvulsantactivitymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis and anticonvulsant activity of some alkanamide derivatives

Tarikogullari

Fatma

Erol

et al. 2011

Arzneimittelforschung

View full text Add to dashboard Cite

show abstract

“…However, several studies suggest that primary metabolites of benzoxazoles are amid derivatives, which form from the hydrolysis of the oxazole ring . As with benzoxazoles, it has been reported that benzamide and phenylacetamide derivatives exhibit various antimicrobial, antiviral, analgesic, anticonvulsant, antihelmintic, and especially anticancer biological properties. Imatinib, structurally a phenyl benzamide derivative, is a well‐known first targeted anticancer agent and a small molecule kinase inhibitor used to treat certain types of cancer.…”

Section: Introductionmentioning

confidence: 99%

Biological evaluation and pharmacophore modeling of some benzoxazoles and their possible metabolites

Zilifdar

Foto

Ertan-Bolelli

et al. 2018

Archiv der Pharmazie

View full text Add to dashboard Cite

A series of benzoxazole derivatives and some possible primary metabolites were evaluated as anticancer agents. In vitro anti-proliferative activities of the compounds were tested using the SRB assay on cancerous (HeLa) and non-cancerous (L929) cell lines. It was found that 17 of 21 tested compounds had cytotoxic activity on HeLa cells and the cytotoxic activities of the compounds were 15-700 times higher than on L929 cells. We generated two distinct pharmacophore models for the cytotoxic activities of the compounds on HeLa and L929 cells. While active compounds such as camptothecin and X8 fitted the two models generated for both cell lines, selective cytotoxic compounds such as XT3B fitted only the model generated for HeLa cells. Evaluation of the genotoxic activities of the cytotoxic compounds with the alkaline comet assay revealed that compounds X17 and XT3 showed strong genotoxic effects against HeLa cells at low concentrations whereas they had no genotoxic effect on L929 cells. Due to the selective ability for inducing DNA strand breaks only on cancerous cells, the compounds were identified as effective derivatives for anticancer candidates.

show abstract

“…The latter 4-nitro-N-phenylbenzamide was also found to be active against seizures induced by scPTZ and was selected for further evaluation in rats dosed orally. In these conditions, N-(2-clhoro-6-methylphenyl)-4-nitrobenzamidc was found to be, three times more active than phenytoin and 4-ainino-N-(2,6-dimethylphenyl) benzamide, two times more potent in the MES test [6]. commercialized in Italy until 1985 with the brand name of Synovial, that has been widely used to treat arthritic patient.…”

Section: Biological Profile Anticonvulsant Activitymentioning

confidence: 99%

Pharmacological Potential of Benzamide Analogues and their Uses in Medicinal Chemistry

Asif¹

2016

Mod Chem Appl

View full text Add to dashboard Cite

Benzamide derivatives possess different kinds of pharmacological activities like antimicrobial, analgesic, antiinflammatory, anticancer, cardiovascular, and other biological activities. Due to these biologically significances, scientists have interesting to develop various new benzamide derivatives. There is still need to improve the already used benzamide derivatives and search for the new and more effective benzamide derivatives. This review exhibited various pharmacophoric activities of benzamides analogues which are biologically importance.

show abstract

Synthesis and anticonvulsant activity of some 4-nitro-N-phenylbenzamides

Cited by 12 publications

References 9 publications

Synthesis and anticonvulsant activity of some alkanamide derivatives

Synthesis and anticonvulsant activity of some alkanamide derivatives

Biological evaluation and pharmacophore modeling of some benzoxazoles and their possible metabolites

Pharmacological Potential of Benzamide Analogues and their Uses in Medicinal Chemistry

Contact Info

Product

Resources

About