Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Design and Synthesis of Novel 2- Substituted Benzothiazole Compounds as PTP1B Inhibitors

Author(s): Arun P. Chandrasekharappa, Sangamesh E. Badiger, Pramod K. Dubey, Sunil K. Panigrahi, Sekhar Reddy VVV. Manukonda.

Graphical Abstract:


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.

Keywords: Benzothiazoles, Oxamic acids, PTP1B, Type 2 Diabetes, pTyr mimetics, Disubstituted sulfonamides.

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Article Details

VOLUME: 11
ISSUE: 4
Year: 2014
Page: [444 - 453]
Pages: 10
DOI: 10.2174/15701808113106660076
Price: $58