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Synthesis, characterization, anti-inflammatory and anti-oxidant activities of novel 2, 4-di substituted 1, 5- benzodiazepine derivatives


Affiliations
1 Department of Pharmaceutical Chemistry, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh., India
2 Department of Chemistry, Vijaya Teja Degree College, Addanki-523201, Andhra Pradesh ., India
3 Department of Pharmaceutics, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh ., India
4 Department of Pharmaceutics, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh., India
5 Department of Pharmaceutical Analysis, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh., India
     

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The study's goal is to synthesis novel benzodiazepine analogues, some of which are chalcones. The elemental analysis, infrared, and 1H nuclear magnetic resonance examinations examined the structures of the newly produced substances. To test for anti-inflammatory and anti-oxidant properties, all substances bearing a descriptor were evaluated. Here, 1,5-(disubstituted phenyl)-2,4-pentadien-1-one derivatives are created from scratch using a new process. By condensing cinnamaldehyde with different aromatic ketones in the presence of 10% NaOH as a base, 1,5-(disubstituted phenyl)-2,4-pentadien-1-one was produced. 2-(substituted phenyl)-3- styryl-2,3-dihydro-1H-benzodiazepine derivatives were synthesised from 1,5-(disubstituted phenyl)-2,4- pentadien-1-one on cyclization with o-phenylene diamine in the presence of NaOH as base. Carrageenan and formalin-induced rat paw edoema technique was used to evaluate the antioxidant and anti-inflammatory activities of the final synthesised benzodiazepine derivatives. Compared to the usual ascorbic acid and diclofenac sodium, the compounds displayed significant anti-inflammatory effect. This means that nitro, chloro, fluoro, and bromo included electron withdrawing groups, which caused an increase in anti-inflammatory action. Most of the produced drugs had strong anti-inflammatory efficacy .

Keywords

Chalcones, 1,5-benzodiazepines, Anti-inflammatory activity, Anti-oxidant activity.
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  • Synthesis, characterization, anti-inflammatory and anti-oxidant activities of novel 2, 4-di substituted 1, 5- benzodiazepine derivatives

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Authors

Nalla Priyanka
Department of Pharmaceutical Chemistry, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh., India
M. Sowjanya
Department of Chemistry, Vijaya Teja Degree College, Addanki-523201, Andhra Pradesh ., India
Miriyala Mrunalini
Department of Pharmaceutics, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh ., India
Ayinam Vasavi
Department of Pharmaceutics, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh., India
G. Raveendra Babu
Department of Pharmaceutical Analysis, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh., India

Abstract


The study's goal is to synthesis novel benzodiazepine analogues, some of which are chalcones. The elemental analysis, infrared, and 1H nuclear magnetic resonance examinations examined the structures of the newly produced substances. To test for anti-inflammatory and anti-oxidant properties, all substances bearing a descriptor were evaluated. Here, 1,5-(disubstituted phenyl)-2,4-pentadien-1-one derivatives are created from scratch using a new process. By condensing cinnamaldehyde with different aromatic ketones in the presence of 10% NaOH as a base, 1,5-(disubstituted phenyl)-2,4-pentadien-1-one was produced. 2-(substituted phenyl)-3- styryl-2,3-dihydro-1H-benzodiazepine derivatives were synthesised from 1,5-(disubstituted phenyl)-2,4- pentadien-1-one on cyclization with o-phenylene diamine in the presence of NaOH as base. Carrageenan and formalin-induced rat paw edoema technique was used to evaluate the antioxidant and anti-inflammatory activities of the final synthesised benzodiazepine derivatives. Compared to the usual ascorbic acid and diclofenac sodium, the compounds displayed significant anti-inflammatory effect. This means that nitro, chloro, fluoro, and bromo included electron withdrawing groups, which caused an increase in anti-inflammatory action. Most of the produced drugs had strong anti-inflammatory efficacy .

Keywords


Chalcones, 1,5-benzodiazepines, Anti-inflammatory activity, Anti-oxidant activity.

References