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    1/25/2012 1

    ANALGESIC EFFECT OF NEW

    SYNTHETIC DRUG BENZOFURAN-3,4-DIHYDROXY CHALCONE BY

    HOT PLATE TESTS IN MICE

    Theresia Ayu. Rayon 2443009070Edwin Jeika B. 2443009108

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    OUTLINE

    Introduction

    Materials Methods

    Results & Disscusion

    Conclusions

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    INTRODUCTION

    Analgesic drugs relief pain

    ??

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    Effiicacy &Unwanted

    Effect

    Need new

    better drugs

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    INTRODUCTION

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    ChalconeDerivates

    Anti-inflammatory effect andcancer chemo preventiveactivity

    Hydroxy chalcones inhibit 12-lipoxygenase & cycloxygenase

    Benzofuran-3-one Derivates

    Anti-inflammatory effectRapidly and extensivelymetabolized after systemicadministration nontoxic

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    INTRODUCTION : Purpose

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    ChalconeDerivates

    DerivatBenzofuran-3-one

    Activity Tests

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    MATERIALs

    Synthesis

    Pharmacology

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    5-MethoxybenzofuranOxalyl ChlorideDiazomethane

    Acetic Acid3,4-DihydroxybenzaldehydeDry HCl

    Mice: Male SwissAlbino

    with good housing

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    METHODs

    Synthesis ofDrugs:

    Reaction &Crystalilzed

    Pharmacology:

    Analgesic Effecttested by Hotplate method

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    O

    O

    O

    Cl

    2,5-dimethoxybenzoyl chloride

    N+

    N-

    diazomethan

    O

    O

    O

    N N

    2-diazo-1-(2,5-dimethoxyphenyl)ethanone

    O

    O

    O

    OH

    2,5-dimethoxybenzoic acid

    O

    O

    Cl

    Cl

    oxalyl dichloride

    O

    O

    O

    Cl

    2,5-dimethoxybenzoyl chloride

    Step 1

    Step 2

    Method: Synthesis

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    O

    O

    O

    N N

    2-diazo-1-(2,5-dimethoxyphenyl)ethanone

    O

    OH

    acetic acid

    O

    O

    O

    5-methoxybenzofuran-3(2H)-one

    O

    O

    O

    5-methoxybenzof uran-3(2H)-one

    O

    OH

    OH

    3,4-dihydroxybenzaldehyde O

    O

    OOH

    OH

    (z)-2-(3,4-dihydroxybenzylidene)-5-methoxybenzofuran-3(2h)-one

    Step 3

    Step 4

    Method: Synthesis

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    Benzofuran-3,4-dihydroxy

    chalcone (BF-DK)

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    Method : Hot Plate

    Temperature 551C

    Observation

    0, 15, 30, 45, and 60 min after i.p.

    lick the fore or hind paw or jump out

    Quantitatif Maximum Possible Effect

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    Method : Hot Plate

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    Group 1 2 3 -controll +controll

    Drug BF-

    DK

    BF-

    DK

    BF-

    DK

    Saline Morphin

    e

    Ibuprofen

    Doses(mg/kg)

    12,5 25 50 10ml/kg 2,5 200

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    RESULT & DISCUSSION

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    RESULT & DISSCUSION

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    RESULT & DISSCUSION

    Concentration of BF-DK, reached to max in

    45 minutes after injection Metabolized

    In acute phase, BF-DK equal to ibuprofen Analgesic effect of Benzofuran-3,4-dihydroxy

    chalcone is lower than Morphine (central

    analgesic)

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    CONCLUSION

    Drug have analgesic effect

    Further research can be developing to

    investigation the analgesic mechanisms ofthe drug

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