Synthesis and biological screening of some novel 3-subsituted indole derivatives

Abstract

In the present work Indole and substituted glycolic acid have been chosen as starting materials. These are broad class of chemical compounds, with many important pharmacological properties. Because of ease of reaction with electrophiles, indole is widely used in various pharmaceutical preparations. The present investigation was concerned with synthesis of some novel 3-substituted indole derivatives with objective of discovery novel and potent analgesic, anti-inflammatory and anti-oxidant agents. These compounds were synthesized by cyclisation of indole-3-acetic acid with different aromatic amines. The structures of new compounds were confirmed by FT IR, 1HNMR and Mass. These compounds were tested in-vivo for analgesic, anti-inflammatory activates and biochemical studies antioxidant activity. The statistical analysis was carried out by ANOVA. All the compounds tested (NHR-I-NHR-VII) showed analgesic, anti-inflammatory and antioxidant activities. Among seven compounds three compounds (NHR-I, NHR-II, NHR-IV) showed significant analgesic, anti-inflammatory and antioxidant activities.Compounds NHR-II and NHR-V showed 74.38% and 70.68% inhibition of paw oedema in anti-inflammatory activity compared to 75.28% inhibition of standard Indomethacin.Compounds NHR-I and NHR-II showed 68.84% and 73.30% inhibition against acetic acid induced writings' in analgesic activity compared to 75.23% inhibition of standard Diclofenac.Compound NHR-II showed 71.6% inhibition of DPPH radical in Anti-oxidant activity compared to 84% inhibition of standard Ascorbic acid. The results showed that incorporation of appropriately substituted aromatic amines at third position of Indole nucleus can afford good analgesic, anti-inflammatory and antioxidant with reduced side effects of compounds.