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 VVV. Manukonda.
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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