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Synthesis and Biological Evaluation of 3-(4-aminophenyl)-2-(1H-indol-3-yl) Propanamide derivatives as novel PTP1B Inhibitors

Author Affiliations

  • 1Medicinal Chemistry, Aurigene Discovery Technologies Ltd, Hosur Road, Bangalore – 560100, INDIA
  • 2Department of Chemistry, JNTUH College of Engineering, Hyderabad - 500085, INDIA

Res.J.chem.sci., Volume 2, Issue (9), Pages 63-71, September,18 (2012)

Abstract

Indole scaffold represents one of the most important subunit explored in medicinal chemistry. We explored the possibilities of using the 3-(4-aminophenyl)-2-(1H-indol-3-yl)propanamide derivatives as PTP1B inhibitors. These inhibitors were designed based on molecular docking studies. Among the prioritized molecule 2-((4-(3-amino-2-(1H-indol-3-yl)-3-oxopropyl) phenyl) amino)-2-oxoacetic acid and their derivatives found to show reasonable potency for PTP1B. These compounds were examined for PTP1B inhibition through in-vitro assay. Best compound 15a showed Ki of 52 µM.

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