We are analyzing https://link.springer.com/article/10.1007/s00044-011-9739-5.

Title:
Synthesis, characterization and pharmacological evaluation of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives as potent anticonvulsant agents | Medicinal Chemistry Research
Description:
A series of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives were synthesized by coupling it with different substituted aldehydes, acetophenone, and benzophenones in presence of absolute ethanol along with catalytic amount of glacial acetic acid. All the synthesized compound were confirmed and characterized by using various spectral technique like IR, 1H NMR, 13C NMR, and mass spectroscopy studies. Anticonvulsant evaluations of all the synthesized compounds were done using various seizures models like maximal electroshock-induced seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) at a dose of 30, 100, and 300 mg/kg body weight and anticonvulsant activity was noted at 0.5 h and 4 h time intervals after the drug administration. Compound 1a (E)-N′-2-benzylidene isonicotinohydrazide, 1g (E)-N′-2-ethoxybenzylidene isonicotinohydrazide, 1k (E)-N′-3-flourobenzylidene isonicotinohydrazide and 3a (E)-N′-diphenylmethylene isonicotinohydrazide showed protection in MES model, which indicates that these compounds have the ability to prevent the spread of seizure at 300 mg/kg dose and showed protection at 0.5 h duration. Compound 3a was also found to be active in scPTZ screen at a dose of 300 mg/kg. In neurotoxicity screen, all the synthesized compounds were found non-toxic except compounds 1n, 2a, and 3b. Further compounds 1a, 1g, 1k, and 3a were also evaluated in the minimal clonic seizure model and exhibited potent anticonvulsant activity with lower neurotoxicity. Among all synthesized derivatives, analogue 3a was found to exhibit protection in MES and scPTZ seizure models. This study proved that isonicotinoyl hydrazides synthesized by condensing isoniazid with various aldehydes and ketones displayed moderate to potent anticonvulsant activity.
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Topics {✒️}

5-chloro-3-methyl-1-phenyl-1h-pyrazol-4-yl month download article/chapter aroyl-hydrazone based ligand maximal electroshock-induced seizure anticonvulsant structure–activity relationships anticonvulsant drug screening 300 mg/kg body weight potent anticonvulsant agents full article pdf dimmock jr aakash deep potential anticonvulsant agents privacy choices/manage cookies antiepileptic drug development 1h-triazol-1-yl potent anticonvulsant activity maximal electroshock dcreen related subjects antiepileptic drugs 4-sulphamoyl phenyl semicarbazones article malhotra benzothiazole-hydrazone derivatives european economic area glacial acetic acid ketones displayed moderate pandeya sn major urinary metabolite rigidified amino acids anti-tubercular activity anti-mycobacterial activity ram-eash institute king saud university maharshi dayanand university chiral gaba analogues gaba uptake inhibitors gaba receptor agonists author correspondence conditions privacy policy mass spectroscopy studies molecular modeling studies subcutaneous pentylenetetrazole methylene]2/4-substituted hydrazides nicotinic acid hydrazone aryl alicyclic ketones accepting optional cookies article log abdul samad isonicotinoyl hydrazides synthesized puthucode rn pharmacological screening

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         headline:Synthesis, characterization and pharmacological evaluation of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives as potent anticonvulsant agents
         description:A series of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives were synthesized by coupling it with different substituted aldehydes, acetophenone, and benzophenones in presence of absolute ethanol along with catalytic amount of glacial acetic acid. All the synthesized compound were confirmed and characterized by using various spectral technique like IR, 1H NMR, 13C NMR, and mass spectroscopy studies. Anticonvulsant evaluations of all the synthesized compounds were done using various seizures models like maximal electroshock-induced seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) at a dose of 30, 100, and 300 mg/kg body weight and anticonvulsant activity was noted at 0.5 h and 4 h time intervals after the drug administration. Compound 1a (E)-N′-2-benzylidene isonicotinohydrazide, 1g (E)-N′-2-ethoxybenzylidene isonicotinohydrazide, 1k (E)-N′-3-flourobenzylidene isonicotinohydrazide and 3a (E)-N′-diphenylmethylene isonicotinohydrazide showed protection in MES model, which indicates that these compounds have the ability to prevent the spread of seizure at 300 mg/kg dose and showed protection at 0.5 h duration. Compound 3a was also found to be active in scPTZ screen at a dose of 300 mg/kg. In neurotoxicity screen, all the synthesized compounds were found non-toxic except compounds 1n, 2a, and 3b. Further compounds 1a, 1g, 1k, and 3a were also evaluated in the minimal clonic seizure model and exhibited potent anticonvulsant activity with lower neurotoxicity. Among all synthesized derivatives, analogue 3a was found to exhibit protection in MES and scPTZ seizure models. This study proved that isonicotinoyl hydrazides synthesized by condensing isoniazid with various aldehydes and ketones displayed moderate to potent anticonvulsant activity.
         datePublished:2011-07-15T00:00:00Z
         dateModified:2011-07-15T00:00:00Z
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            Neurotoxicity
            Pharmacology/Toxicology
            Biochemistry
            general
            Medicinal Chemistry
            Bioorganic Chemistry
            Inorganic Chemistry
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      headline:Synthesis, characterization and pharmacological evaluation of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives as potent anticonvulsant agents
      description:A series of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives were synthesized by coupling it with different substituted aldehydes, acetophenone, and benzophenones in presence of absolute ethanol along with catalytic amount of glacial acetic acid. All the synthesized compound were confirmed and characterized by using various spectral technique like IR, 1H NMR, 13C NMR, and mass spectroscopy studies. Anticonvulsant evaluations of all the synthesized compounds were done using various seizures models like maximal electroshock-induced seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) at a dose of 30, 100, and 300 mg/kg body weight and anticonvulsant activity was noted at 0.5 h and 4 h time intervals after the drug administration. Compound 1a (E)-N′-2-benzylidene isonicotinohydrazide, 1g (E)-N′-2-ethoxybenzylidene isonicotinohydrazide, 1k (E)-N′-3-flourobenzylidene isonicotinohydrazide and 3a (E)-N′-diphenylmethylene isonicotinohydrazide showed protection in MES model, which indicates that these compounds have the ability to prevent the spread of seizure at 300 mg/kg dose and showed protection at 0.5 h duration. Compound 3a was also found to be active in scPTZ screen at a dose of 300 mg/kg. In neurotoxicity screen, all the synthesized compounds were found non-toxic except compounds 1n, 2a, and 3b. Further compounds 1a, 1g, 1k, and 3a were also evaluated in the minimal clonic seizure model and exhibited potent anticonvulsant activity with lower neurotoxicity. Among all synthesized derivatives, analogue 3a was found to exhibit protection in MES and scPTZ seizure models. This study proved that isonicotinoyl hydrazides synthesized by condensing isoniazid with various aldehydes and ketones displayed moderate to potent anticonvulsant activity.
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      dateModified:2011-07-15T00:00:00Z
      pageStart:2145
      pageEnd:2152
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         Isoniazid
         (E)-N′-(substituted-benzylidene)isonicotinohydrazide
         Anticonvulsant
         Pentylenetetrazole
         Neurotoxicity
         Pharmacology/Toxicology
         Biochemistry
         general
         Medicinal Chemistry
         Bioorganic Chemistry
         Inorganic Chemistry
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      name:Department of Pharmaceutical Chemistry, Ram-Eash Institute of Technical and Vocational Studies, Greater Noida, India
      name:Department of Pharmaceutical Chemistry, College of Pharmacy in Al-Kharj, King Saud University, Riyadh, Saudi Arabia
      name:Preclinical Pharmacology, National Institute of Neurological Disorders and Stroke (NINDS), National Institute of Health (NIH), Bethesda, USA
      name:Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India
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