Abstract
Some 6-Phenyl/Biphenyl-4-yl-2-[2-(pyridin-2-ylamino)-ethyl]/-2-(2N-subtituted amin-1-yl)-ethyl-4,5- dihydropyridazin-3(2H)-one (4a-h) were synthesized by reacting 6-phenyl/biphenyl-4,5-dihydropyridazin-3(2H)-one with bromoethyl derivatives of cyclic secondary amines and 2-aminopyridine. All the compounds, 4a-h, were evaluated as anticonvulsant by using maximum electro shock (MES) and isoniazid (INH) induced convulsion methods at 50mg/kg dose level, and as antitubercular by Microplate Almar Blue Assay (MABA) method. In anticonvulsant activity, phenytoin (25mg/kg) and sodium vaproate (50mg/kg) were used as reference drugs. All compounds (4a-h) showed significant anticonvulsant activities against both MES and INH methods, and compound g showed highest activity against MES method. In antitubercular activity, compounds 4c-4h showed 25 μg/ml MIC value, and compounds 4a-4b exhibited 50 µg/ml MIC value when compared with reference drugs [isoniazid (3.125 µg/ml), pyrizinamide (3.125µg/ml)] and (streptomycin 6.25μg/ml) MIC values, and found less potent than the reference drugs.
Keywords: Anticonvulsant, Antitubercular, Biological activities, Heterocyclic, Pyridazinone, Synthetic compounds.
Letters in Drug Design & Discovery
Title:Anticonvulsant and Antitubercular Activities of 6-Phenyl/Biphenyl-4-yl-2- [2-(pyridin-2-ylamino)-ethyl]- and 6-(Biphenyl-4yl)-2-(2N-subtituted amin- 1-yl)-ethyl derivatives of 4,5-dihydropyridazin-3(2H)-one
Volume: 10 Issue: 7
Author(s): Mohammad Asif, Anita Singh, Lakshmayya, Asif Husain and Anees A. Anees
Affiliation:
Keywords: Anticonvulsant, Antitubercular, Biological activities, Heterocyclic, Pyridazinone, Synthetic compounds.
Abstract: Some 6-Phenyl/Biphenyl-4-yl-2-[2-(pyridin-2-ylamino)-ethyl]/-2-(2N-subtituted amin-1-yl)-ethyl-4,5- dihydropyridazin-3(2H)-one (4a-h) were synthesized by reacting 6-phenyl/biphenyl-4,5-dihydropyridazin-3(2H)-one with bromoethyl derivatives of cyclic secondary amines and 2-aminopyridine. All the compounds, 4a-h, were evaluated as anticonvulsant by using maximum electro shock (MES) and isoniazid (INH) induced convulsion methods at 50mg/kg dose level, and as antitubercular by Microplate Almar Blue Assay (MABA) method. In anticonvulsant activity, phenytoin (25mg/kg) and sodium vaproate (50mg/kg) were used as reference drugs. All compounds (4a-h) showed significant anticonvulsant activities against both MES and INH methods, and compound g showed highest activity against MES method. In antitubercular activity, compounds 4c-4h showed 25 μg/ml MIC value, and compounds 4a-4b exhibited 50 µg/ml MIC value when compared with reference drugs [isoniazid (3.125 µg/ml), pyrizinamide (3.125µg/ml)] and (streptomycin 6.25μg/ml) MIC values, and found less potent than the reference drugs.
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Asif Mohammad, Singh Anita, Lakshmayya , Husain Asif and Anees A. Anees, Anticonvulsant and Antitubercular Activities of 6-Phenyl/Biphenyl-4-yl-2- [2-(pyridin-2-ylamino)-ethyl]- and 6-(Biphenyl-4yl)-2-(2N-subtituted amin- 1-yl)-ethyl derivatives of 4,5-dihydropyridazin-3(2H)-one, Letters in Drug Design & Discovery 2013; 10 (7) . https://dx.doi.org/10.2174/1570180811310070013
DOI https://dx.doi.org/10.2174/1570180811310070013 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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