Abstract

The objective of the paper was to design, synthesis and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and evaluate for anti-inflammatory potential. The 1,3,5-tri-substituted-2-pyrazolines derivatives has been synthesized by the reaction of chalcone derivatives with 4-hydrazinylbenzene sulfonamide hydrochloride and phenyl hydrazine hydrochloride. Total Sixteen compounds has been synthesized and characterized by the IR, 1HNMR and mass spectral analysis. Proposed compounds have been evaluated for anti-inflammatory activity. Anti-inflammatory activity of the compounds carried out by two animal model i.e. Carrageenan induced, paw edema in rats and Inhibition of formalin induced paw edema in rats. Anti-inflammatory activity of the compounds C7, C8 and C2 were shown 98.26, 92.77 and 96.24 percentages of inhibition and compounds D7, D8 and D2 were shown 81.50, 83.81 and 78.32 percentages of inhibition as compared to the standard drug Diclofenac at 10 mg/kg was inhibit the inflammation 99.42 % after 6h. These result is a evident that synthesized compounds show relevant degree of anti-inflammatory activity as compared to the standard drug. It is also concluded that the presence of SO2NH2 group, Cl, CH3, OCH3 and N(CH3)2 group may provide the active compounds when attached to the pyrazoline group. But the addition of OH, Br and no substitution in phenyl ring may diminish the activity.

Highlights

  • Pyrazole has a chemical behaviour that is unusual not just among heterocyclic compounds, and among related azoles [1]

  • The synthesised chalcone derivatives were combined in absolute alcohol with equimolar amounts of 4-hydrazinylbenzene sulfonamide hydrochloride and phenyl hydrazine hydrochloride (0.005M) and a little amount of pyridine and POCl3 (0.01M) (5-7 ml)

  • The similar technique was followed, in which chalcone derivatives interacted with the phenyl hydrazine hydrochloride

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Summary

INTRODUCTION

Pyrazole has a chemical behaviour that is unusual not just among heterocyclic compounds, and among related azoles [1] This is because pyrazole has the normal aromatic system features, which are really rather prominent in these derivatives, as well as the high ring liability under specific conditions. The study of chemical properties, the peculiarities of the behaviour of pyrazole derivatives and the clarification of their physicochemical features, has recently gotten a lot of interest. This allowed for the collection of fresh data that was crucial. The objective of the paper was to design, synthesis and characterization of new 1,3,5- trisubstituted- 2- pyrazolines derivative and evaluate for anti-inflammatory potential

MATERIALS AND METHODS
Synthesis scheme-II
Anti-inflammatory activity
Anti-inflammatory properties
Animal grouping and dose planning
Experimental Procedure
Screening for Anti-inflammatory
Inhibition of formalin induced paw edema in rats
Spectral Analysis
Compound C2
Compound C6
3.1.10 Compound D2
3.1.11 Compound D3
Compound D1
3.1.13 Compound D5
3.1.14 Compound D6
3.1.15 Compound D7
3.1.16 Compound D8
Inhibition of Formalin Induced Paw Edema in Rats
Anti-inflammatory Properties
Carrageenan Induced Paw Edema in Rat Model
Formalin Induced Paw Edema in Rat Model
Findings
Kavitha

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