Synthesis and evaluation of some novel dibenzo [b, d] furan carboxylic acids as potential anti-diabetic agents

…, YR Prasad, L Gharat, A Thomas, S Narayanan…

文献索引：Lakshminarayana; Prasad, Y. Rajendra; Gharat, Laxmikant; Thomas, Abraham; Narayanan, Shridhar; Raghuram; Srinivasan; Gopalan, Balasubramanian European Journal of Medicinal Chemistry, 2010 , vol. 45, # 9 p. 3709 - 3718

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被引用次数: 21

摘要

A series of novel dibenzo [b, d] furan mono-carboxylic acid derivatives were synthesized, characterized and evaluated for their ability to inhibit Protein Tyrosine Phosphatase 1B (PTP1B) in vitro in order to use them as potential anti-diabetic agents. Structure–activity relationship study led to the identification of potent compound 5E which inhibited PTP1B with IC50 value of 82±0.43 nM. Compound 5E was screened in vivo as drug candidate for ...