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

18 Citations (Scopus)

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
Externally publishedYes

Fingerprint

Oxamic Acid
Benzoxazoles
Molecular modeling
Structure-Activity Relationship

Keywords

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

ASJC Scopus subject areas

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

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

Design and synthesis of 2-substituted benzoxazoles as novel PTP1B inhibitors. / Chandrasekharappa, Arun P.; Badiger, Sangamesh E.; Dubey, Pramod K.; Panigrahi, Sunil K.; Manukonda, Sekhar Reddy V V V.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 23, No. 9, 01.05.2013, p. 2579-2584.

Research output: Contribution to journalArticle

Chandrasekharappa, AP, Badiger, SE, Dubey, PK, Panigrahi, SK & Manukonda, SRVVV 2013, 'Design and synthesis of 2-substituted benzoxazoles as novel PTP1B inhibitors', Bioorganic and Medicinal Chemistry Letters, vol. 23, no. 9, pp. 2579-2584. https://doi.org/10.1016/j.bmcl.2013.02.109
Chandrasekharappa AP, Badiger SE, Dubey PK, Panigrahi SK, Manukonda SRVVV. Design and synthesis of 2-substituted benzoxazoles as novel PTP1B inhibitors. Bioorganic and Medicinal Chemistry Letters. 2013 May 1;23(9):2579-2584. https://doi.org/10.1016/j.bmcl.2013.02.109
Chandrasekharappa, Arun P. ; Badiger, Sangamesh E. ; Dubey, Pramod K. ; Panigrahi, Sunil K. ; Manukonda, Sekhar Reddy V V V. / Design and synthesis of 2-substituted benzoxazoles as novel PTP1B inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2013 ; Vol. 23, No. 9. pp. 2579-2584.
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