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Synthesis and Evaluation of Some Novel Dibenzo[b,d]furan Carboxylic Acids as Potential Anti-Diabetic Agents

N Lakshminarayana, Y Rajendra Prasad, Laxmikant Gharat, Abraham Thomas, Shridhar Narayanan, A Raghuram, C V Srinivasan, Balasubramanian Gopalan

Eur J Med Chem. 2010 Sep;45(9):3709-18.

PMID: 20627471

Abstract:

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 5 E which inhibited PTP1B with IC(50) value of 82+/-0.43 nM. Compound 5 E was screened in vivo as drug candidate for anti-diabetic activity using rosiglitazone maleate as the standard. Compound 5 E showed significant reduction in body weight, fed-state whole blood glucose (WBG), fasting WBG, plasma glucose and plasma cholesterol levels and non-significant reduction in fasting plasma triglyceride levels in ob/ob mice.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AS23102 Maleate Standard for IC Maleate Standard for IC Price
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