Synthesis and anticonvulsant activity of 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues

doi:10.3109/14756366.2012.663364

Paper

Synthesis and anticonvulsant activity of 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues

Published Jan 29, 2013 · M. Ahsan, Habibullah Khalilullah, J. Stables

Journal of Enzyme Inhibition and Medicinal Chemistry

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Abstract

A series of fourteen 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues were synthesized and evaluated for anticonvulsant activity according to the Antiepileptic Drug Development Programme (ADD) protocol. Some of the synthesized compounds showed significant activity in minimal clonic seizure model (6 Hz psychomotor seizure test). 3-(4-Fluorophenyl)-N-(4-bromophenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide (4c) was found to be the most active compound of the series showing 75% (3/4, 0.25–2.0 h) and 50% (2/4, 4.0 h) protection against minimal clonic seizure at 100 mg/kg without any toxicity. 3-(Pyridin-4-yl)-N-(4-chlorophenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide (4f) showed protection in maximal electroshock (MES) seizure and subcutaneous metrazol (scMET) seizure at 300 mg/kg.

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Study Snapshot

3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues show significant anticonvulsant activity, with 4c showing 75% protection against minimal clonic seizure and 4f showing protection in maximal electro

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and anticonvulsant activity of 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues

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References

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Aryl acid hydrazones of nicotinic acid hydrazide show potential as a new pharmacophore for designing novel anticonvulsant drugs.

Synthesis and antimycobacterial evaluation of 3a,4-dihydro-3H-indeno [1,2-c] pyrazole-2-carboxamide analogues.

The synthesized compounds show low to good inhibitory activities against Mycobacterium tuberculosis H37 Rv and MDR-TB, with 3-(4-fluorophenyl)-N-(4-chlorophenyl)-6,7-dimethoxy-3a,4

Discovery of novel antitubercular 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues.

The synthesized compounds show promising antitubercular activity against Mycobacterium tuberculosis H(37)Rv and isoniazid resistant M. tuberculosis, with 3-(4-fluorophenyl)-6,7-dimethoxy-3a,4-d

Design, synthesis and antimycobacterial evaluation of novel 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues.

Novel 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues show moderate to high inhibitory activities against Mycobacterium tuberculosis

Synthesis of N 1 -(3-chloro-4-flourophenyl)- N 4 -substituted semicarbazones as novel anticonvulsant agents

Compound 3i, N1-(3-chloro-4-fluorophenyl)-N4-(4-N,N-dimethylamino-benzaldehyde) semicarbazone, shows promising anticonvulsant activity without neurotoxicity and less CNS depress

Citations

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