Design and synthesis of 2-substituted benzoxazoles as novel PTP1B inhibitors

Arun P. Chandrasekharappa, Sangamesh E. Badiger, Pramod K. Dubey, Sunil K. Panigrahi, Sekhar Reddy V.V.V. Manukonda

Research output: Contribution to journalArticle

19 Scopus citations

Abstract

A series of benzoxazole compounds containing oxamic acid were synthesized and screened for the PTP1B inhibition. Compound 31d showed best biochemical potency (Ki) of 6.7 μM. Structure-activity relationship were explained with the help of molecular modeling approach.

Original languageEnglish (US)
Pages (from-to)2579-2584
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number9
DOIs
StatePublished - May 1 2013

Keywords

  • Benzimidazole
  • Benzoxazole
  • Diabetes
  • Oxamic acids
  • PTP1B
  • pTyr mimetics

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Chandrasekharappa, A. P., Badiger, S. E., Dubey, P. K., Panigrahi, S. K., & Manukonda, S. R. V. V. V. (2013). Design and synthesis of 2-substituted benzoxazoles as novel PTP1B inhibitors. Bioorganic and Medicinal Chemistry Letters, 23(9), 2579-2584. https://doi.org/10.1016/j.bmcl.2013.02.109