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.
Letters in Drug Design & Discovery
Title:Design and Synthesis of Novel 2- Substituted Benzothiazole Compounds as PTP1B Inhibitors
Volume: 11 Issue: 4
Author(s): Arun P. Chandrasekharappa, Sangamesh E. Badiger, Pramod K. Dubey, Sunil K. Panigrahi and Sekhar Reddy VVV. Manukonda
Affiliation:
Keywords: Benzothiazoles, Oxamic acids, PTP1B, Type 2 Diabetes, pTyr mimetics, Disubstituted sulfonamides.
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.
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Cite this article as:
Chandrasekharappa P. Arun, Badiger E. Sangamesh, Dubey K. Pramod, Panigrahi K. Sunil and Manukonda Reddy VVV. Sekhar, Design and Synthesis of Novel 2- Substituted Benzothiazole Compounds as PTP1B Inhibitors, Letters in Drug Design & Discovery 2014; 11 (4) . https://dx.doi.org/10.2174/15701808113106660076
DOI https://dx.doi.org/10.2174/15701808113106660076 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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