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

European Journal of Medicinal Chemistry
N LakshminarayanaBalasubramanian Gopalan

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.

Citations

Jul 24, 2012·The FEBS Journal·Rongjun HeZhong-Yin Zhang
Oct 6, 2015·Trends in Pharmacological Sciences·Zhong-Yin ZhangTony Tiganis
Apr 29, 2016·European Journal of Medicinal Chemistry·Peihong LiuQunyi Li
Feb 5, 2019·Current Topics in Medicinal Chemistry·Phaedra EleftheriouAnthi Petrou
Oct 17, 2018·Mini Reviews in Medicinal Chemistry·Garima VermaMohammad Shaquiquzzaman
Jul 25, 2019·Current Molecular Pharmacology·Ajay KumarRohit Bhatia
Sep 2, 2020·European Journal of Medicinal Chemistry·Antonios KousaxidisAthina Geronikaki

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