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Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH3 or 2-CH3

Agnieszka Gunia-Krzyżak, Dorota Żelaszczyk, Anna Rapacz, Ewa Żesławska, more

Bioorganic & Medicinal Chemistry > 2017 > 25 > 2 > 471-482

A series of twenty two (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH₃ or 2-CH₃ was designed, synthesized and evaluated for anticonvulsant activity in rodent models of seizures: maximal electroshock (MES) test, subcutaneous pentylenetetrazole (scPTZ) test, and 6-Hz test. There were identified three most active compounds: S-(2E)-N-(1-hydroxypropan-2-yl)-3-(2-methylphenyl)prop-2-enamide...

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Design, Synthesis, and Biological Evaluation of 6‐(2‐Amino‐substituted phenyl)‐4‐(substituted phenyl)‐1,2,4‐triazine‐3,5(2H,4H)‐dione Derivatives as Anticonvulsant Agents

Ahsan Ahmed Khan, Nadeem Siddiqui, Md. Jawaid Akhtar, Zulphikar Ali, more

Archiv der Pharmazie > 349 > 4 > 277 - 292

As per structural requirement essential for anticonvulsant activity, a series of new 6‐(2‐amino‐substituted phenyl)‐4‐(substituted phenyl)‐1,2,4‐triazine‐3,5‐dione derivatives were designed and synthesized. All the synthesized title derivatives were assessed for in vivo anticonvulsant screening by the two most employed standard animal seizure models, maximal electroshock seizure (MES) and subcutaneous...

article

Synthesis and Pharmacological Evaluation of Novel 1′‐[2‐(Difluoromethoxy)benzyl]‐2′H,5′H‐spiro[8‐azabicyclo[3.2.1]octane‐3,4′‐imidazolidine]‐2′,5′‐diones and Their Derivatives

Malavalli Madaiah, Maralekere K. Prashanth, Hosakere D. Revanasiddappa, Bantal Veeresh

Archiv der Pharmazie > 347 > 5 > 370 - 380

A series of novel 1′‐[2‐(difluoromethoxy)benzyl]‐2′H,5′H‐spiro[8‐azabicyclo[3.2.1]octane‐3,4′‐imidazolidine]‐2′,5′‐dione substituted hydantoins (5–32) were synthesized using an appropriate synthetic route and characterized by elemental analysis and spectral data. The novel molecules were screened for anticonvulsant activity in mice by maximal electroshock (MES) and subcutaneous pentylenetetrazol (ScPTZ)‐induced...

article

Enaminones 12. An explanation of anticonvulsant activity and toxicity per Linus Pauling’s clathrate hypothesis

Patrice L. Jackson, Clive D. Hanson, Alanna K. Farrell, Raymond J. Butcher, more

European Journal of Medicinal Chemistry > 2012 > 51 > Complete > 42-51

The x-ray crystal structure of 3-((5-methylisoxazol-3-yl)amino)-5-methylcyclohex-2-enone (12b) and 3-((5-methylisoxazolyl-3-yl)amino)-5,5-dimethylcyclohex-2-enone (12c) were determined and correlated to their anticonvulsant activity in mice and rats. A hypothesis for the toxicity of the analogs are advanced. In addition, a series of 5-methyl-N-(3-oxocyclohex-1-enyl)-isoxazole-3-carboxamides were synthesized...

article

Design and Synthesis of Novel Diphenyl Oxalamide and Diphenyl Acetamide Derivatives as Anticonvulsants

Anna Pratima G. Nikalje, Mangesh Ghodke, Amol Girbane

Archiv der Pharmazie > 345 > 1 > 57 - 64

A series of novel N¹‐substituted‐N²,N²‐diphenyl oxalamides 3a–l were synthesized in good yield by stirring diphenylcarbamoyl formyl chloride (2) and various substituted aliphatic, alicyclic, aromatic, heterocyclic amines in DMF and K₂CO₃. Also 2‐substituted amino‐N,N‐diphenylacetamides 5a–m were designed by pharmacophore generation and synthesized by stirring 2‐chloro‐N,N‐diphenylacetamide (4) and...

article

Nicotinic acid hydrazones: a novel anticonvulsant pharmacophore

Reema Sinha, U. V. Singh Sara, R. L. Khosa, James Stables, more

Medicinal Chemistry Research > 2011 > 20 > 9 > 1499-1504

A series of aryl acid hydrazones of substituted aromatic acid hydrazides (D ₁ to D ₂₀) were synthesised and evaluated for anticonvulsant activity. Aryl acid hydrazones of Nicotinic acid hydrazide (D ₈, D ₉, and D ₁₀) have displayed excellent protection in maximal electroshock screen. These compounds have also exhibited excellent binding properties with Lys 329 residue of gamma amino butyrate amino...

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Anticonvulsant and Toxicity Evaluation of Newer 4H‐Benzo[1,4]oxazin‐3‐ones: The Effect of Two Hydrogen Bonding Domains

Nadeem Siddiqui, Ruhi Ali, M. Faiz Arshad, Waquar Ahsan, more

Archiv der Pharmazie > 343 > 11‐12 > 657 - 663

A series of (Z)‐2‐(substituted aryl)‐N‐(3‐oxo‐4‐(substituted carbamothioyl)‐3,4‐dihydro‐2H‐benzo[b][1,4]oxazin‐7‐yl) hydrazine carboxamides (6a–r) was synthesized using 2‐amino‐5‐nitrophenol as a starting material. All the synthesized compounds possessed two hydrogen‐bonding domains and their effect on the activity was studied thereof. The anticonvulsant activity was assessed by the maximal electroshock...

article

Enaminones 8: CoMFA and CoMSIA studies on some anticonvulsant enaminones

Patrice L. Jackson, K.R. Scott, William M. Southerland, Ya-Yin Fang

Bioorganic & Medicinal Chemistry > 2009 > 17 > 1 > 133-140

3D-QSAR studies comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were carried out on 26 structurally diverse subcutaneous pentylenetetrazol (scPTZ) active enaminone analogues, previously synthesized in our laboratory. CoMFA and CoMSIA were employed to generate models to define the specific structural and electrostatic features essential for...

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Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH3 or 2-CH3

Design, Synthesis, and Biological Evaluation of 6‐(2‐Amino‐substituted phenyl)‐4‐(substituted phenyl)‐1,2,4‐triazine‐3,5(2H,4H)‐dione Derivatives as Anticonvulsant Agents

Synthesis and Pharmacological Evaluation of Novel 1′‐[2‐(Difluoromethoxy)benzyl]‐2′H,5′H‐spiro[8‐azabicyclo[3.2.1]octane‐3,4′‐imidazolidine]‐2′,5′‐diones and Their Derivatives

Enaminones 12. An explanation of anticonvulsant activity and toxicity per Linus Pauling’s clathrate hypothesis

Design and Synthesis of Novel Diphenyl Oxalamide and Diphenyl Acetamide Derivatives as Anticonvulsants

Nicotinic acid hydrazones: a novel anticonvulsant pharmacophore

Anticonvulsant and Toxicity Evaluation of Newer 4H‐Benzo[1,4]oxazin‐3‐ones: The Effect of Two Hydrogen Bonding Domains

Enaminones 8: CoMFA and CoMSIA studies on some anticonvulsant enaminones

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