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Abstract

PHARMACOLOGICAL STUDY OF BIOTRANSFORMATION OF SUBSTITUTED AND UNSUBSTITUTED INDANONE ACETIC ACID ADDUCT WITH PYRAZOLONE RING FOR ANALGESIC ACTIVITY IN-VIVO

Substituted and unsubstituted indanone acetic acids have been synthesized and conjugated with carboxy-pyrazolone to get indanonepyrazolone adduct. The antiinflammatory activity has been screened for Indanone acetic acid, Indanone-Pyrazolone adduct and Carboxy Pyrazolone by rat paw edema method with reference standard drug Indomethacin which is bioisosteres with indanone acetic acid ring. It has been observed that all the test compounds have anti-inflammatory activity and 70% inhibition of edema persists for 3 hours in the case of Indanone acetic acids and for Carboxy pyrazolone and 60-70% inhibition of edema persists for 5 hours in the case of Indanone-pyrazolone adduct. Indanone has non-heterocyclic fused ring having six membered benzene ring and five membered cyclopentane ring where as pyrazolone has five membered heterocyclic ring substituted with six membered benzene ring. The adduct of indanone acetic acid and carboxy pyrazolone joins with amide linkage which has free carboxy group which is present in the both Indanone acetic acid and Carboxy pyrazolone. Indanone-pyrazolone adduct shows high lipid solubility by partition coefficient rather than the other two compounds which shows the same % inhibition of edema and longer duration of analgesic activity which is equal to the other test compounds. It proves that the Indanone-Pyrazolone adduct shows activity for a certain period and then releases the two factors Indanone acetic acid and Carboxy Pyrazolone after hydrolysis of amide linkage by biotransformation in-vivo and the activity becomes prolonged but the % inhibition remains the same due to the in-vivo synergism appears and the combination activity of the three shows more prolonged action with longer duration by competitive inhibition of arachidonic acid pathway which has also free carboxylic acid group


Author(s): NIRALI A PASSI, MAULIK K PRAJAPATI, PROF DR DHRUBO JYOTI SEN AND PROF DR INDERMEET SINGH ANAND

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