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In vitro and in silico evaluation of chromene based aroyl hydrazones as anticonvulsant agents

Violina T. Angelova, Yulian Voynikov, Pavlina Andreeva-Gateva, Slavina Surcheva, more

Medicinal Chemistry Research > 2017 > 26 > 9 > 1884-1896

Series of aroyl hydrazones of 2H-chromene and coumarin carbaldehydes were synthesized and evaluated for their anticonvulsant activity and neurotoxicity. Further docking study on gamma-aminobutyric acid receptor was performed to elucidate their mechanisms of action. The highest protection was demonstrated by 2-furyl substituted 2H-chromene 8b in the maximal electroshock test (ED₅₀ = 12.51 mg kg⁻¹,...

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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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6-HZ (2)
MES (2)
ANTICONVULSANT (1)
CINNAMAMIDE (1)
COUMARIN (1)
CRYSTAL STRUCTURE (1)
DOCKING (1)
HYDRAZONES (1)
PHARMACOPHORE (1)
PTZ (1)
SCPTZ (1)
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In vitro and in silico evaluation of chromene based aroyl hydrazones as anticonvulsant agents

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

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