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Design and synthesis of 2-substituted benzoxazoles as novel PTP1B inhibitors
Authors:Arun P. Chandrasekharappa  Sangamesh E. Badiger  Pramod K. Dubey  Sunil K. Panigrahi  Sekhar Reddy V.V.V. Manukonda
Affiliation:1. Aurigene Discovery Technologies Limited, 39-40, KIADB Industrial Area, Phase II, Electronic City, Hosur Road, Bangalore 560 100, India;2. Department of Chemistry, JNTUH College of Engineering, Hyderabad 500 085, India
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.
Keywords:Benzimidazole  Benzoxazole  Oxamic acids  PTP1B  Diabetes  pTyr mimetics
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