Synthesis and biological evaluation of some N-substituted indole analogues

Abstract

The esterification of 1-alkyl/aryl-3-ethoxy carbonyl-5-hydroxy-2-methyl indoles (1a-g) with ethyl chloroacetate and ethyl chloroformate, afforded ethyl 5-(ethoxycarbonyl) methoxy]-1-alkyl/aryl-2-methyl-indole-3-carboxylate (2a-g) and 3-(ethoxycarbonyl)-1-alkyl/aryl-2-methyl-1H-indol-5-yl ethyl carbonate (3a-g) respectively. The reaction of 1b-g with monochloroacetic acid and 2-chloropropionic acid afforded the corresponding indole acetic acid (4b-g) and propanoic acid (5b-g) derivatives respectively. These newly synthesized compounds were evaluated in vivo for potential anti-inflammatory and analgesic activities and the results were compared with indomethacin. These analogues were administered p.o. at a dose level of 20 mg/kg.

Regioselective synthesis of novel 2,3,4,4a-tetrahydro-1H-carbazoles and their cholinesterase inhibitory activities

“…7,8 Thus, the need for novel anti-Alzheimer's agents driven us to evaluate novel indoletype derivatives as cholinesterase inhibitors. Indole derivatives have inspired chemists due to their natural origin and diverse pharmacological properties, [9][10][11] such as neuroprotective, 12 glucokinase, 13 anti-oxidant, 14 anti-cancer 15 etc. Besides these activities, the indole scaffold is also considered as a promising target for cholinesterase inhibition.…”

Crack detection and localization in RC beams through smart MWCNT/epoxy strip-like strain sensors

“…In addition, damages are not isolated crack-like but smeared cracks in the areas subjected to tensile stresses. The studied beam is retrieved from [62] and has a cross-section of 25 cm width, 45 cm depth, and the beam is 400 cm long, with an effective span of 380 cm. The longitudinal reinforcement consists of two rebars of 16 mm diameter in the bottom part of the beam, and two rebars of 10 mm diameter in the upper part of the beam.…”

Synthesis, Molecular Docking and Biological Evaluation of N‐Substituted Indole Derivatives as Potential Anti‐Inflammatory and Antioxidant Agents

“…Literature on the N-ethyl substituted indole derivatives with good anti-inflammatory and antioxidant activity is also available. [22,23] Inflammation is a complex reaction of the body to harmful stimuli, i. e., pathogens, damaged cells, and irritants. Inflammation is involved in tissue repair.…”

“…It would be a great strategy to conjugate hetero‐cyclic moieties with indole to get superior and potent derivatives. Literature on the N ‐ethyl substituted indole derivatives with good anti‐inflammatory and antioxidant activity is also available [22,23] …”