Abstract

A REVIEW OF ANTI INFLAMMATORY POTENTIAL OF INDOLE AND ITS DERIVATIVES

Mahesh Patel, Varsha Kashaw, Anita Devi Shivhare*, Vineeta Devi Shivhare

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Abstract

Indole is a privileged heterocyclic nucleus set up in diverse natural products, endogenous molecules and medicinal agents. Even though it has diversified actions, the role of indole in anti-inflammatory therapy is of prime interest which is prominently shown in the drug molecule Indomethacin. The efficacy of the indomethacin and tenidap is primarily due to the inhibition of the cyclooxygenase (COX) enzyme activity. The adverse reactions of most of the NSAIDs (Non Steroidal Antiinflammatory Drugs) are due to the irritating moiety present in the molecule or due to the decreased production of cytoprotective prostaglandins. In this review, the various structural modifications of indole have been studied to enlist the improvement in the therapeutic profile of the nucleus. A new series of 1,5-disubstituted indole derivatives such as 5-(acetylamino)-1-[(4- flurophenyl)carbonyl]-1H-indole-3-carboxylicacid, 1-[(4 fluorophenyl)carbonyl]-5- [(phenylcarbonyl)amino]-1H-indole-3-carboxylic acid, 1-(4-flurobenzoyl)-5-(4- ethylbenzamido-1H- indole-3-carboxylic acid, 5-(4-nitrobenzamido)-1-(4-flurobenzoyl)-1Hindole- 3-carboxylic acid, 5-(4- bromobenzamido)-1-(4-flurobenzoyl)-1H-indole-3-carboxylic acid were synthesized. All the newly synthesized derivatives of 1,5-disubstituted indole derivatives are characterized by spectroscopically and analytically, Indole containing isoxazole derivatives were reported by Pedada et al. as sPLA2 inhibitory agents. Compound N-((3-(4-fluoro-3-(trifluoromethyl) phenyl) isoxazol-5-yl) methyl) (5-methyl- 1H-indol-3-yl) methanamine hydro- chloride (28) showed significant sPLA2 inhibition activity that is comparable or more to ursolic acid (positive con- trol).

Keywords: Inflammation, Anti-inflammatory Agents, Indole derivatives, Resonance in indole molecule, indomethacin, Modern synthesis of indomethacin.