Design and synthesis of novel 2- substituted benzothiazole compounds as 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

4 Scopus citations

Abstract

Protein tyrosine phosphatase 1B (PTP1B) is a well known drug target for the treatment of type 2 diabetes mellitus (T2DM). Diverse inhibitors have been reported in literature that inhibit PTP1B. We have reported 2-substituted benzoxazole class of In PTP1B inhibitors earlier. Present work describes 2-substituted benzothiazole compounds as PTP1B inhibitor as an extension of our previous study. Compound 23c, a disubstituted para-Bromobenzyl sulfonamide compound, exhibited moderate biochemical potency (Ki) of 1.4 μM. SAR on synthesized compounds was explained using molecular modeling study.

Original languageEnglish (US)
Pages (from-to)444-453
Number of pages10
JournalLetters in Drug Design and Discovery
Volume11
Issue number4
DOIs
StatePublished - May 2014

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Keywords

  • Benzothiazoles
  • Disubstituted sulfonamides
  • Oxamic acids
  • PTP1B
  • PTyr mimetics
  • Type 2 Diabetes

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery

Cite this

Chandrasekharappa, A. P., Badiger, S. E., Dubey, P. K., Panigrahi, S. K., & Manukonda, S. R. V. V. V. (2014). Design and synthesis of novel 2- substituted benzothiazole compounds as PTP1B inhibitors. Letters in Drug Design and Discovery, 11(4), 444-453. https://doi.org/10.2174/15701808113106660076